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Structural Basis of Conformational Dynamics in the PROTAC‐Induced Protein Degradation ChemMedChem (IF 3.4) Pub Date : 2024-04-24 Hongtao Zhao
Pronounced conformational dynamics is unveiled upon analyzing multiple crystal structures of the same proteins recruited to the same E3 ligases by PROTACs, and yet, is largely permissive for targeted protein degradation due to the intrinsic mobility of E3 assemblies creating a large ubiquitylation zone. Mathematical modelling of ternary dynamics on ubiquitylation probability confirms the experimental
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Lysophosphatidic acid receptor 1 (LPA1) antagonists as potential migrastatics for triple negative breast cancer ChemMedChem (IF 3.4) Pub Date : 2024-04-22 Wenjie Liu, Amr Abdullah Kamel Mousa, Austin M Hopkins, Yin Fang Wu, Kelsie L Thu, Michael Campbell, Simon J Lees, Rithwik Ramachandran, Jinqiang Hou
Metastasis is responsible for about 90% of cancer deaths. Anti‐metastatic drugs, termed as migrastatics, offer a distinctive therapeutic approach to address cancer migration and invasion. However, therapeutic exploitation of metastasis‐specific targets remains limited, and the effective prevention and suppression of metastatic cancer continue to be elusive. Lysophosphatidic acid receptor 1 (LPA1) is
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Exploring Raloxifene‐based Metallodrugs: A Versatile Vector Combined with Pt(II), Palladium(II) and Nickel(II) Dichlorides and Carborates against Triple‐Negative Breast Cancer ChemMedChem (IF 3.4) Pub Date : 2024-04-20 Aleksandr Kazimir, Tom Götze, Peter Lönnecke, Blagoje Murganić, Sanja Mijatović, Danijela Maksimović-Ivanić, Evamarie Hey-Hawkins
Triple‐negative breast cancer (TNBC) poses challenges in therapy due to the absence of target expression such as estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER2). Frequently, the treatment of TNBC involves the combination of several therapeutics. However, an enhanced therapeutic effect can be also achieved within a single molecule. The efficacy
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Rational Design and Synthesis of Isatin‐Chalcone Hybrids Integrated with 1H‐1,2,3‐Triazole: Anti‐proliferative Profiling and Molecular Docking Insights ChemMedChem (IF 3.4) Pub Date : 2024-04-19 Vipan Kumar, Swati Swati, Asif Raza, Shefali Chowdhary, Amit Anand, Shaveta Shaveta, Arun Sharma, Kewal Kumar
In this study, a series of isatin‐chalcone linked triazoles were synthesized using Cu‐promoted Azide‐Alkyne Cycloaddition (CuAAC) reaction and evaluated for their cytotoxicity against various cancer cell lines. The most potent compound displayed approximately 2.5 times greater activity compared to both reference compounds against ovarian cancer cell lines. These findings were supported by caspase‐mediated
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Front Cover: Challenges for the Discovery of Non-Covalent WRN Helicase Inhibitors (ChemMedChem 8/2024) ChemMedChem (IF 3.4) Pub Date : 2024-04-19 Alisa Heuser, Wassim Abdul Rahman, Elisabeth Bechter, Jutta Blank, Sylvia Buhr, Dirk Erdmann, Patrizia Fontana, Fanny Mermet-Meillon, Marco Meyerhofer, Ross Strang, Maxime Schrapp, Catherine Zimmermann, Marta Cortes-Cros, Henrik Möbitz, Jacques Hamon
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Developing Low Molecular Weight PET and SPECT Imaging Agents ChemMedChem (IF 3.4) Pub Date : 2024-04-18 Lian Xue, Caitlin V. M. L. Jie, Sandrine Desrayaud, Yves P. Auberson
Imaging agents for positron emission tomography (PET) and single‐photon emission computerized tomography (SPECT) have shown their utility in many situations, answering clinical questions related to drug development and medical considerations. The discovery and development of imaging agents follow a well‐understood process, with variations related to available starting points and to the envisaged imaging
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Surface functionalized titanium nitride electrode for CMOS compatible bioelectronic devices ChemMedChem (IF 3.4) Pub Date : 2024-04-18 Meng Yu, Xiaohui Tang, Shijia Yang, Zhenhua Li, Chang Chen, Sijia Xie
In this study, a surface functionalization approach by covalent grafting of an organic thin film containing hydroxyl groups on TiN surface via electroreduction of diazonium salts "4‐(2‐hydroxyethyl)benzenediazonium salt" is presented. Cyclic voltammetry procedures were carried out at the potential ranges of ‐0.8 V~0.5 V (vs Ag/AgCl) with varying numbers of potential cycles (i.e., 5, 25, and 50 cycles)
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Recent Development of Transition Metal Complexes as Chemotherapeutic Hypoxia Activated Prodrug (HAP) ChemMedChem (IF 3.4) Pub Date : 2024-04-18 K. Jagathesan, SOVAN ROY
Hypoxia is a state characterized by low concentration of Oxygen. Hypoxic state is often found in the central region of solid tumors. Hypoxia is associated with abnormal neovascularization resulted in poor blood flow in tissues and increased proliferation of tumor cells, imbalance between O2 supply and O2 consumption in tumor cells, high concentration of proton and strong reducibility. And, these abnormalities
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Structure and Activity of Reconstructed Pseudo‐Ancestral Cyclotides ChemMedChem (IF 3.4) Pub Date : 2024-04-18 Zhihao Jiang, Yen-Hua Huang, Quentin Kaas, David J. Craik, Conan K. Wang
Cyclotides are cyclic peptides that are promising scaffolds for the design of drug candidates and chemical tools. However, despite there being hundreds of reported cyclotides, drug design studies have commonly focussed on a select few prototypic examples. Here, we explored whether ancestral sequence reconstruction could be used to generate new cyclotides for further optimization. We show that the reconstructed
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Esterification of Cyclic N6‐threonylcarbamoyladenosine during RNA Sample Preparation ChemMedChem (IF 3.4) Pub Date : 2024-04-17 Larissa Bessler, Jason Sirleaf, Christopher J. Kampf, Katarzyna Frankowska, Grażyna Leszczyńska, Till Opatz, Mark Helm
The continuous deciphering of crucial biological roles of RNA modifications and their involvement in various pathological conditions, together with their key roles in the use of RNA‐based therapeutics, has reignited interest in studying the occurrence and identity of non‐canonical ribonucleoside structures during the past years. Discovery and structural elucidation of new modified structures is usually
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Russell Mechanism‐Mediated Cancer Therapy: A Minireview ChemMedChem (IF 3.4) Pub Date : 2024-04-17 Rufeng Zhang, Xiaoyang Liu, Fu-Gen Wu
The Russell mechanism, proposed by Russell, is a cyclic mechanism for the formation of linear tetroxide intermediates, which can spontaneously produce cytotoxic singlet oxygen (1O2) independent of oxygen, suggesting its anticancer potential. Compared with other mainstream anticancer strategies, the Russell mechanism employed for killing cancer cells does not require external energy input, harsh pH
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Nucleic Acid Materials‐mediated Innate Immune Activation for Cancer Immunotherapy ChemMedChem (IF 3.4) Pub Date : 2024-04-16 Xinyu Xu, Yuxuan Hong, Huanhuan Fan, Zijian Guo
Abnormally localized nucleic acids (NAs) are considered as pathogen associated molecular patterns (PAMPs) in innate immunity. They are recognized by NAs‐specific pattern recognition receptors (PRRs), leading to the activation of associated signaling pathways and subsequent production of type I interferons (IFNs) and pro‐inflammatory cytokines, which further trigger the adaptive immunity. Notably, NAs‐mediated
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Front Cover: Identification of ß‐Glucocerebrosidase Activators for Glucosylceramide hydrolysis (ChemMedChem 7/2024) ChemMedChem (IF 3.4) Pub Date : 2024-04-16 Monika‐Sarah E. D. Schulze, Diana Scholz, Eric Jnoff, Adrian Hall, Jonathan Melin, Zara A. Sands, Elizabeth Rodriguez, Veronique M. Andre
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Discovery and in vitro Evaluation of Novel Serotonin 5‐HT2A Receptor Ligands Identified Through Virtual Screening ChemMedChem (IF 3.4) Pub Date : 2024-04-15 Agata Zięba, Damian Bartuzi, Piotr Stępnicki, Dariusz Matosiuk, Tomasz M. Wróbel, Tuomo Laitinen, Marián Castro, Agnieszka Anna Kaczor
The 5‐HT2A receptor is a molecular target of high pharmacological importance. Ligands of this protein, particularly atypical antipsychotics, are useful in the treatment of numerous mental disorders, including schizophrenia and major depressive disorder. Structure‐based virtual screening using a 5‐HT2A receptor complex was performed to identify novel ligands for the 5‐HT2A receptor, serving as potential
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Chemists Invent Drugs and Drugs Save Lives ChemMedChem (IF 3.4) Pub Date : 2024-04-15 Donald F. Weaver
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N,N‐Diarysulfonamide reduces proinflammatory cytokine interleukin‐6 levels in cells through nuclear factor‐κB regulation ChemMedChem (IF 3.4) Pub Date : 2024-04-13 Dattatraya Babar, Gopinath Khansole, Vishalkumar Singh, Akash Shinde, Vaishnavi Kambhampati, Sai Balaji Andugulapati, Haridas B. Rode
The synthesized sulfonamides were evaluated for cytotoxicity followed by the cytokine/inflammatory marker’s inhibition capability and its mechanism of action in RAW‐264.7 cells. Elevated interleukin‐6 (IL‐6) levels have been reported in inflammatory conditions and inflammation‐associated disorders. Hence, reducing the IL‐6 levels in inflammatory conditions can serve as an attractive therapeutic target
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Small‐Molecule Allosteric Inhibitors of Human Aspartate Transcarbamoylase Suppress Proliferation of Bone Osteosarcoma Epithelial Cells ChemMedChem (IF 3.4) Pub Date : 2024-04-11 Chao Wang, Bidong Zhang, Yingying Cong, Xiaochen Du, Siyao Chen, Lidia Visser, Angel Ruiz-Moreno, Lili Zhang, Fulvio Reggiori, Domling Alexander, Matthew Robert Groves
Aspartate transcarbamoylase (ATC) is the first committed step in de novo pyrimidine biosynthesis in eukaryotes and plants. A potent transition state analog of human ATCase (PALA) has previously been assessed in clinical trials for the treatment of cancer, but was ultimately unsuccessful. Additionally, inhibition of this pathway has been proposed to be a target to suppress cell proliferation in E. coli
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Chemical derivatization leads to the discovery of novel analogs of azotochelin, a natural siderophore, as promising anticancer agents ChemMedChem (IF 3.4) Pub Date : 2024-04-10 Nishant M. Karadkhelkar, Pranav Gupta, Leonard Barasa, Rameswari Chilamakuri, Christopher K. Hlordzi, Nikita Acharekar, Saurabh Agarwal, Zhe-Sheng Chen, Sabesan Yoganathan
Siderophores are structurally unique medicinal natural products and exhibit considerable therapeutic potential. Herein, we report the design and synthesis of azotochelin, a natural siderophore, and an extensive library of azotochelin analogs as a potential anticancer agent. We modified the carboxylic acid and the aromatic ring motifs of azotochelin using various chemical motifs. We tested the compounds
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Application of an NMR/crystallography fragment screening platform for the assessment and rapid discovery of new HIV‐CA binding fragments ChemMedChem (IF 3.4) Pub Date : 2024-04-06 Stuart Lang, Dan A Fletcher, Alain-Pierre Petit, Nicola Luise, Paul K Fyfe, Fabio Zuccotto, David Porter, Anthony Hope, Fiona Bellany, Catrina Kerr, Claire J MacKenzie, Paul G Wyatt, David W. Gray
Identification and assessment of novel targets is essential to combat drug resistance in the treatment of HIV/AIDS. HIV Capsid (HIV‐CA), the protein playing a major role in both the early and late stages of the viral life cycle, has emerged as an important target. We have applied an NMR fragment screening platform and identified molecules that bind to the N‐terminal domain (NTD) of HIV‐CA at a site
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Chemical and Chemoenzymatic Synthesis of Peptide and Protein Therapeutics Conjugated with Human N‐Glycans ChemMedChem (IF 3.4) Pub Date : 2024-04-04 Hirofumi Ochiai, Sofia Elouali, Takahiro Yamamoto, Hiroaki Asai, Masato Noguchi, Yuji Nishiuchi
Glycosylation is one of the most ubiquitous post‐translational modifications. It affects the structure and function of peptides/proteins and consequently has a significant impact on various biological events. However, the structural complexity and heterogeneity of glycopeptides/proteins caused by the diversity of glycan structures and glycosylation sites complicates the detailed elucidation of glycan
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Potent Anthelmintic Activity of Chalcones Synthesized by an Effective Green Approach ChemMedChem (IF 3.4) Pub Date : 2024-04-04 Ornella Turani, M. Julia Castro, Juliana Vazzana, Pamela Mendioroz, María A. Volpe, Darío C. Gerbino, Cecilia Bouzat
There is currently an urgent need for new anthelmintic agents due to increasing resistance to the limited available drugs. The chalcone scaffold is a privileged structure for developing new drugs and has been shown to exhibit potential antiparasitic properties. We synthesized a series of chalcones via Claisen‐Schmidt condensation, introducing a novel recoverable catalyst derived from biochar obtained
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Benzofurans as acetylcholinesterase inhibitors for treating Alzheimer's disease: synthesis, in vitro testing, and in silico analysis ChemMedChem (IF 3.4) Pub Date : 2024-03-30 Arturo Coaviche-Yoval, Ricardo Tovar-Miranda, Jessica E. Rodríguez, Jesus A. Lagos-Cruz, Héctor Luna, Erik Andrade-Jorge, José Guadalupe Trujillo-Ferrara
: Alzheimer’s disease (AD) is a neurodegenerative disorder and the leading cause of dementia worldwide. It is characterized by a progressive decline in cholinergic neurotransmission. During the development of AD, acetylcholinesterase (AChE) binds to β‐amyloid peptides to form amyloid fibrils, which aggregate into plaque deposits. These complexes are cytotoxic for the brain, causing impairment of memory
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Auto‐Cleaving Bond for Better Drugs ChemMedChem (IF 3.4) Pub Date : 2024-03-30 Jiaqi Guo, Annabelle Chang, Bing Xu
While bond formation has historically been the mainstay of medicinal chemistry, the phenomenon of bond cleavage has received less focus. However, the success of numerous oral medications demonstrates the importance of controlled cleavage in prodrugs to achieve desired therapeutic outcomes. Nevertheless, effective strategies to control this cleavage remain limited. This concept article introduces a
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Finding the ajoene sweet‐spot: structure‐activity relations that govern its blood stability and cancer cytotoxicity ChemMedChem (IF 3.4) Pub Date : 2024-03-27 Daniel A Kusza, Gerhard A Venter, Mandla Mabunda, James Biwi, Suman K. Samanta, Johan D Klinck, Shivendra V Singh, Roger Hunter, Catherine H Kaschula
Ajoene is an organosulfur compound found in crushed garlic, that exerts its anti‐cancer activity by S‐thiolating cysteine residues on proteins. Its development is hampered due to limited bioavailability. In this study, we synthesised analogues of ajoene to probe the significance of the ajoene vinyl disulfide/sulfoxide core with respect to cytotoxicity and blood stability. Polar side groups were also
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Welcoming Our New Editorial Advisory Board Chairs ChemMedChem (IF 3.4) Pub Date : 2024-03-26 David Peralta
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Front Cover: Structural Development of Androgen Receptor Antagonists Using Phenylferrocene Framework as a Hydrophobic Pharmacophore (ChemMedChem 6/2024) ChemMedChem (IF 3.4) Pub Date : 2024-03-26 Kotaro Ochiai, Ryo Yonezawa, Shinya Fujii
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Uracil‐ and Pyridine‐Containing HDAC Inhibitors Displayed Cytotoxicity in Colorectal and Glioblastoma Cancer Stem Cells ChemMedChem (IF 3.4) Pub Date : 2024-03-26 Francesco Fiorentino, Emanuele Fabbrizi, Alessia Raucci, Beatrice Noce, Rossella Fioravanti, Sergio Valente, Chantal Paolini, Ruggero De Maria, Christian Steinkühler, Paola Gallinari, Dante Rotili, Antonello Mai
Cancer stem cells (CSCs) are a niche of highly tumorigenic cells featuring self‐renewal, activation of pluripotency genes, multidrug resistance, and ability to cause cancer relapse. Seven HDACi (1‐7), showing either hydroxamate or 2'‐aminoanilide function, were tested in colorectal cancer (CRC) and glioblastoma multiforme (GBM) CSCs to determine their effects on cell proliferation, H3 acetylation levels
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Structural analysis of the macrocyclic inhibitor BI‐4020 binding to EGFR kinase ChemMedChem (IF 3.4) Pub Date : 2024-03-25 Tyler S Beyett, Jaimin K Rana, Ilse K Schaeffner, David E Heppner, Michael Eck
A novel macrocyclic inhibitor of mutant EGFR (BI‐4020) has shown promise in pre‐clinical studies of T790M and C797S drug‐resistant non‐small cell lung cancer. To better understand the molecular basis for BI‐4020 selectivity and potency, we have carried out biochemical activity assays and structural analysis with X‐ray crystallography. Biochemical potencies agree with previous studies indicating that
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C9-Functionalized Doxycycline Analogs as Drug Candidates to Prevent Pathological α-Synuclein Aggregation and Neuroinflammation in Parkinson's Disease Degeneration ChemMedChem (IF 3.4) Pub Date : 2024-03-25 Clémence Rose, Rodrigo Hernán Tomas-Grau, Brenda Zabala, Patrick Pierre Michel, Jean-Michel Brunel, Rosana Chehín, Rita Raisman-Vozari, Laurent Ferrié, Bruno Figadère
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Developing Dynamic Structure‐Based Pharmacophore and ML‐Trained QSAR Models for the Discovery of Novel Resistance‐Free RET Tyrosine Kinase Inhibitors ChemMedChem (IF 3.4) Pub Date : 2024-03-25 Ehsan Sayyah, Lalehan Oktay, Hüseyin Tunç, Serdar Durdagi
Activation of RET tyrosine kinase plays a critical role in the pathogenesis of various cancers, including non‐small cell lung cancer, papillary thyroid cancers, multiple endocrine neoplasia type 2A and 2B (MEN2A, MEN2B), and familial medullary thyroid cancer. Gene fusions and point mutations in the RET proto‐oncogene result in constitutive activation of RET signaling pathways. Consequently, developing
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Phosphine-Catalyzed Synthesis and Cytotoxic Evaluation of Michael Adducts of the Sesquiterpene Lactone Arglabin ChemMedChem (IF 3.4) Pub Date : 2024-03-22 Alexey V. Salin, Andrey A. Shabanov, Khasan R. Khayarov, Daut R. Islamov, Alexandra D. Voloshina, Syumbelya K. Amerhanova, Anna P. Lyubina
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Development of benzimidazole‐substituted spirocyclopropyl oxindole derivatives as cytotoxic agents: tubulin polymerization inhibition and apoptosis inducing studies ChemMedChem (IF 3.4) Pub Date : 2024-03-22 Akash P. Sakla, Mohd Rabi Bazaz, Ashutosh Mahale, Pravesh Sharma, Durgesh Gurukkala Valapil, Onkar Prakash Kulkarni, Manoj P. Dandekar, Nagula Shankaraiah
A series of spirocyclopropyl oxindoles with benzimidazole substitutions was synthesized and tested for their cytotoxicity against selected human cancer cells. Most of the molecules exhibited significant antiproliferative activity with compound 12p being the most potent. It exhibited significant cytotoxicity against MCF‐7 breast cancer cells (IC50 value 3.14 ± 0.50 µM), evidenced by the decrease in
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Natural distribution, structures, synthesis, and bioactivity of hasubanan alkaloids ChemMedChem (IF 3.4) Pub Date : 2024-03-20 Yingjie Wang, Fuxin Sun, Yapeng Liang, Di Zhou, Gang Chen, Ning Li
Hasubanan alkaloids represent a distinct class of alkaloids bearing a structural resemblance to morphine, predominantly found in herbals of the Stephania genus. Their intriguing molecular architecture and potential analgesic properties have captured the interest of medicinal chemists worldwide. This review meticulously examines the natural distribution, structural characteristics, biosynthetic pathways
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Iodinated 4,4’-Bipyridines with Antiproliferative Activity Against Melanoma Cell Lines ChemMedChem (IF 3.4) Pub Date : 2024-03-15 Paola Peluso, Victor Mamane, Ylenia Spissu, Giuseppina Casu, Alessandro Dessì, Roberto Dallocchio, Barbara Sechi, Giuseppe Palmieri, Carla Rozzo
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Discovery of Potent Isoindolinone Inhibitors that Target an Active Conformation of PARP1 Using DNA-Encoded Libraries ChemMedChem (IF 3.4) Pub Date : 2024-03-14 Kelly A. McCarthy, Douglas J. Marcotte, Sangram Parelkar, Crystal L. McKinnon, Lindsay E. Trammell, Eric L. Stangeland, Rachael R. Jetson
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Medical Applications of Silver and Gold Nanoparticles and Core-Shell Nanostructures Based on Silver or Gold Core: Recent Progress and Innovations ChemMedChem (IF 3.4) Pub Date : 2024-03-13 Agata Kowalska, Elżbieta Adamska, Beata Grobelna
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Targeted Redox Balancing through Pulmonary Nanomedicine Delivery Reverses Oxidative Stress Induced Lung Inflammation ChemMedChem (IF 3.4) Pub Date : 2024-03-08 Ria Ghosh, Monojit Das, Susmita Mondal, Amrita Banerjee, Lopamudra Roy, Anjan Kumar Das, Debasish Pal, Siddhartha Sankar Bhattacharya, Maitree Bhattacharyya, Samir Kumar Pal
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Identification of Potential Inhibitors of the SARS-CoV-2 NSP13 Helicase via Structure-Based Ligand Design, Molecular Docking and Nonequilibrium Alchemical Simulations ChemMedChem (IF 3.4) Pub Date : 2024-03-08 Giorgio Di Paco, Marina Macchiagodena, Piero Procacci
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Spiro-Acridine Compound as a Pteridine Reductase 1 Inhibitor: in silico Target Fishing and in vitro Studies ChemMedChem (IF 3.4) Pub Date : 2024-03-06 Jéssika de Oliveira Viana, Marina Sena Mendes, Marcelo Santos Castilho, Ricardo Olímpio de Moura, Euzébio Guimarães Barbosa
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Combinatorial Libraries of Bipodal Binders of the Insulin Receptor ChemMedChem (IF 3.4) Pub Date : 2024-03-06 Irena Selicharová, Benjamin Fabre, María Soledad Garre Hernández, Marta Lubos, Jan Pícha, Zdeněk Voburka, Katarína Mitrová, Jiří Jiráček
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Copper and Copper Complexes in Tumor Therapy ChemMedChem (IF 3.4) Pub Date : 2024-03-05 Yingqiao Wang, Tingxi Tang, Yi Yuan, Nan Li, Xiaoqing Wang, Jian Guan
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Front Cover: Design Principles for Balancing Lipophilicity and Permeability in beyond Rule of 5 Space (ChemMedChem 5/2024) ChemMedChem (IF 3.4) Pub Date : 2024-03-02 Henrik Möbitz
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Design, Synthesis, and Biological Evaluation of Eukaryotic Initiation Factor 2B (eIF2B) Activators ChemMedChem (IF 3.4) Pub Date : 2024-03-01 Yifeng Pei, Sentao Liu, Lixun Wang, Chao Chen, Mengqiu Hu, Yi Xue, Dezhong Guan, Lingfeng Xie, Hong Liao, Jinpei Zhou, Huibin Zhang
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Chimeric Amphiphilic Disinfectants: Quaternary Ammonium/Quaternary Phosphonium Hybrid Structures ChemMedChem (IF 3.4) Pub Date : 2024-02-28 Moneya S. Leatherbury, Laura M. Thierer, Christian A. Sanchez, Germán G. Vargas-Cuebas, Ashley A. Petersen, Lauren E. Amoo, Elise L. Bezold, Keshyne C. Washington, M. Brody Mistrot, Michael J. Zdilla, William M. Wuest, Kevin P. C. Minbiole
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The amphipathic design in helical antimicrobial peptides ChemMedChem (IF 3.4) Pub Date : 2024-02-26 Hai Bui Thi Phuong, Hoa Doan Ngan, Binh Le Huy, Hoang Vu Dinh, Huy Luong Xuan
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Small Molecule-Drug Conjugates: Opportunities for the Development of Targeted Anticancer Drugs ChemMedChem (IF 3.4) Pub Date : 2024-02-23 Jingjing Zhang, Fanchun Hu, Omer Aras, Yichao Chai, Feifei An
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Inducing Targeted Protein Degradation: From Chemical Biology to Drug Discovery and Clinical Applications. Edited by Philipp Cromm ChemMedChem (IF 3.4) Pub Date : 2024-02-22 Kirsten McAulay
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Fragment-Based Design, Synthesis, and Characterization of Aminoisoindole-Derived Furin Inhibitors ChemMedChem (IF 3.4) Pub Date : 2024-02-22 Roman W. Lange, Konstantin Bloch, Miriam Ruth Heindl, Jan Wollenhaupt, Manfred S. Weiss, Hans Brandstetter, Gerhard Klebe, Franco H. Falcone, Eva Böttcher-Friebertshäuser, Sven O. Dahms, Torsten Steinmetzer
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Identification of ß-Glucocerebrosidase Activators for Glucosylceramide hydrolysis ChemMedChem (IF 3.4) Pub Date : 2024-02-21 Monika-Sarah E. D. Schulze, Diana Scholz, Eric Jnoff, Adrian Hall, Jonathan Melin, Zara A. Sands, Elizabeth Rodriguez, Veronique M. Andre
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Accelerating BRPF1b hit identification with BioPhysical and Active Learning Screening (BioPALS) ChemMedChem (IF 3.4) Pub Date : 2024-02-19 Sandeep Pal, Zandile Nare, Vincenzo A. Rao, Brian O. Smith, Ian Morrison, Edward A. Fitzgerald, Andrew Scott, Matilda J. Bingham, Thomas Pesnot
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Investigating the Combined Toxicity of Cu(II) and Carbon Monoxide (CO); Cellular CO Delivery Using a Cu(II) Flavonolato Complex ChemMedChem (IF 3.4) Pub Date : 2024-02-18 Stephen N. Anderson, C. Taylor Dederich, Josiah G. D. Elsberg, Abby D. Benninghoff, Lisa M. Berreau
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Front Cover: r-BRICS – A Revised BRICS Module That Breaks Ring Structures and Carbon Chains (ChemMedChem 4/2024) ChemMedChem (IF 3.4) Pub Date : 2024-02-16 Leili Zhang, Vasumitra Rao, Wendy Cornell
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Helical BODIPY Dyes as Heavy-Atom-Free Triplet Photosensitizers for Photodynamic Therapy of Cancer ChemMedChem (IF 3.4) Pub Date : 2024-02-15 Soumyaditya Mula, Mrunesh Koli
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Tailored Tetrasubstituted Imidazole Carrying the Benzenesulfonamide Fragments as Selective Human Carbonic Anhydrase IX/XII Inhibitors ChemMedChem (IF 3.4) Pub Date : 2024-02-15 Ehab S. Taher, Adel A. Marzouk, Walaa Hamada Abd-Allah, Simone Giovannuzzi, Tarek S. Ibrahim, Claudiu T. Supuran, Mohamed A. El Hamd, Mohammed Farrag El-Behairy
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Nano-Engineering Strategies for Tumor-Specific Therapy ChemMedChem (IF 3.4) Pub Date : 2024-02-14 Zijin Li, Hai-Yan Xie, Weidong Nie
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Compounds Consisting of Quinazoline, Ibuprofen, and Amino Acids with Cytotoxic and Anti-Inflammatory Effects ChemMedChem (IF 3.4) Pub Date : 2024-02-14 Luis Roberto Garduño-Villavicencio, Ulises Martínez-Ortega, Elizabeth Ortiz-Sánchez, José Manuel Tinajero-Rodríguez, Francisco Hernández-Luis
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Insights into the Overcoming EGFRDel19/T790M/C797S Mutation: A Perspective on the 2-aryl-4-aminothienopyrimidine Backbone ChemMedChem (IF 3.4) Pub Date : 2024-02-14 Xuan Zhang, Jie He, Shidi Xu, Li Fu, Pengwu Zheng, Shan Xu, Qingshan Pan, Wufu Zhu
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A Structure-Activity Relationship Study of Amino Acid Derivatives of Pterostilbene Analogues Toward Human Breast Cancer ChemMedChem (IF 3.4) Pub Date : 2024-02-12 Fabiana Cordella, Nicola Dragone, Rosarita D'Orsi, Concetta Saponaro, Daniele Vergara, Marco Lessi, Gaetano Angelici
Pterostilbene is the dimethylated analogue of Resveratrol, a compound with well-known biological activities, such as antioxidant, chemopreventive, anti-diabetic, anti-obesity, and cardioprotective. Despite many studies on the general effect of such polyphenolic molecules and their derivatives, a deep comprehension of their action and systematic structure-activity relationship studies are still rare
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Diversity Oriented Synthesis of Novel Xanthones Reveal Potent Doxorubicin-Inspired Analogs ChemMedChem (IF 3.4) Pub Date : 2024-02-13 Jonas W. Meringdal, Leon Bade, Gerd Bendas, Dirk Menche
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Neuroblastoma and its Target Therapies: A Medicinal Chemistry Review ChemMedChem (IF 3.4) Pub Date : 2024-02-10 A. Gerges, U. Canning