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hERG, Plasmodium Life Cycle, and Cross Resistance Profiling of New Azabenzimidazole Analogues of Astemizole ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-17 Dickson Mambwe, Dina Coertzen, Meta Leshabane, Mwila Mulubwa, Mathew Njoroge, Liezl Gibhard, Gareth Girling, Kathryn J. Wicht, Marcus C. S. Lee, Sergio Wittlin, Diogo Rodrigo Magalhães Moreira, Lyn-Marie Birkholtz, Kelly Chibale
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Design, Synthesis, and Evaluation of 8-(o-Tolyl)quinazoline Derivatives as Small-Molecule PD-1/PD-L1 Antagonists ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-15 Xingye Wu, He Li, Han Liu, Xueyan Ding, Xinting Chen, Chenxi Yin, Yali Gao, Junjie Ma
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Chemical Space Profiling of SARS-CoV-2 PLpro Using DNA-Encoded Focused Libraries ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-14 Xudong Wang, Ying Zhu, Qingyi Zhao, Weiwei Lu, Yechun Xu, Hangchen Hu, Xiaojie Lu
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Discovery of a New Class of 1-(4-Sulfamoylbenzoyl)piperidine-4-carboxamides as Human Carbonic Anhydrase Inhibitors ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-13 Davide Moi, Serena Vittorio, Andrea Angeli, Claudiu T. Supuran, Valentina Onnis
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Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable In Vivo Studies: Discovery of TDI-11055 ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-12 Mayako Michino, Tanweer A. Khan, Michael W. Miller, Yoshiyuki Fukase, Jeremie Vendome, Carolina Adura, J. Fraser Glickman, Yiman Liu, Liling Wan, C. David Allis, Andrew W. Stamford, Peter T. Meinke, Louis M. Renzetti, Stacia Kargman, Nigel J. Liverton, David J. Huggins
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Exploring Scaffold Hopping for Novel 2-(Quinolin-4-yloxy)acetamides with Enhanced Antimycobacterial Activity ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-11 Ana Flávia Borsoi, Alessandro Silva Ramos, Nathalia Sperotto, Bruno Lopes Abbadi, Fernanda Souza Macchi Hopf, Adilio da Silva Dadda, Raoní Scheibler Rambo, Mauro Neves Muniz, Josiane Delgado Paz, Estevão Silveira Grams, Fernanda Fries da Silva, Kenia Pissinate, Luiza Galina, Laura Calle González, Lovaine Silva Duarte, Marcia Alberton Perelló, Alexia de Matos Czeczot, Cristiano Valim Bizarro, Luiz Augusto
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Novel Phosphorylpurinone Compounds for Treating Cancer ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-08 Ram W. Sabnis
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Novel PCSK9 Inhibitors for Treating Cardiovascular Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-08 Ram W. Sabnis
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Empowering Voices: Inspiring Women in Medicinal Chemistry ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-08 Maria-Jesus Blanco, Joanne J. Bronson, Erin F. DiMauro, Carolyn Dzierba, MariJean Eggen, Amanda L. Garner, Gunda Georg, Jeanine Giarolla, Nicole C. Goodwin, Melissa C. Grenier-Davies, Carrie Haskell-Luevano, Ulrike Holzgrabe, Rong Huang, H. Rachel Lagiakos, Katerina Leftheris, Yvonne Martin, Maria João Matos, Tricia L. May-Dracka, Christa E. Müller, Amy H. Newman, Emma Parmee, Jennifer C. Petter, Nuria
As we celebrate International Women’s Day 2024 with the theme “Inspire Inclusion”, the women of the ACS Medicinal Chemistry Division (MEDI) want to foster a sense of belonging, relevance, and empowerment by sharing uplifting stories of what inspired them to become medicinal chemists. In this editorial, we are featuring female medicinal chemistry scientists to provide role models, encouragement, and
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Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-07 Stefan McCarver, Luke Hanna, Andrew Samant, Aaron A. Thompson, Mark Seierstad, Arjun Saha, Dongpei Wu, Brian Lord, Steven W. Sutton, Vishal Shah, Cynthia M. Milligan, Michelle Wennerholm, Jonathan Shelton, Terry P. Lebold, Brock T. Shireman
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Identification of Dual Inhibitors Targeting Main Protease (Mpro) and Cathepsin L as Potential Anti-SARS-CoV-2 Agents ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-01 Santo Previti, Roberta Ettari, Elsa Calcaterra, Michele Roggia, Benito Natale, Annabelle C. Weldert, Christin Müller-Ruttloff, Florian Salisch, Anna Irto, Rosalia Maria Cigala, John Ziebuhr, Tanja Schirmeister, Sandro Cosconati, Maria Zappalà
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Novel-Type GABAB PAMs: Structure–Activity Relationship in Light of the Protein Structure ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-03-01 Balázs Krámos, Zsuzsa Hadady, Attila Makó, Gábor Szántó, Nóra Felföldi, Ildikó Magdó, Amrita Ágnes Bobok, Imre Bata, Viktor Román, András Visegrády, György M. Keserű, István Greiner, János Éles
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Combination of Allosteric and Orthosteric EGFR Inhibitors for Treating Non-Small-Cell Lung Cancer ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-27 Ram W. Sabnis
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Tips for Getting Your Manuscript Accepted into ACS Medicinal Chemistry Letters ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-27 John G. Woodland, Kelly Chibale
Scientific publications are the culmination of the scientific enterprise, providing the foundation for new hypotheses and technologies. A good paper, written for and by researchers, clearly and convincingly presents the findings of a carefully conducted study to the larger scientific community. Scientific publications also yield indirect rewards; for example, they may advance a researcher’s career
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Novel Heterocyclic PAD4 Inhibitors for Treating Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-27 Ram W. Sabnis
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Forging a Future Free from Neglected Tropical Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-26 Flavio da Silva Emery, Kelly Chibale
World Neglected Tropical Diseases Day (“World NTD Day”), established by the World Health Organization and observed every January 30th, raises awareness and mobilizes action against neglected tropical diseases (NTDs), affecting over 1.6 billion people worldwide. (1,2) In recent years, we have witnessed advances in the development of tools to control, prevent, and eliminate at least one NTD in many countries
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Forgotten Natural Products: Semisynthetic Development of Blasticidin S As an Antibiotic Lead ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-23 Cole Gannett, Kateland Tiller, Anthony J. Briganti, Anne M. Brown, James Weger-Lucarelli, Andrew N. Lowell
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Design, Synthesis, and Antifungal Activity of 3-Substituted-2(5H)-Oxaboroles ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-22 Rose Campbell, Nicklas W. Buchbinder, Connor Szwetkowski, Yumeng Zhu, Karla Piedl, Mindy Truong, John B. Matson, Webster L. Santos, Emily Mevers
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64Cu-Labeled Boron-Containing Cyclic RGD Peptides for BNCT and PET Imaging ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-21 Soyeon Kim, Sajid Mushtaq, Kyo Chul Lee, Ji Ae Park, Jung Young Kim
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Probing the Use of Triphenyl Phosphonium Cation for Mitochondrial Nucleoside Delivery ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-15 Mathis Guiraud, Lamiaa M. A. Ali, Emma Gabrieli-Magot, Laure Lichon, Morgane Daurat, David Egron, Magali Gary-Bobo, Suzanne Peyrottes
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ZX703: A Small-Molecule Degrader of GPX4 Inducing Ferroptosis in Human Cancer Cells ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-15 Mengdie Hu, Xiaomei Li, Lin Wang, Yanping Zhang, Yujie Sun, Hui Hua, Huina Liu, Ting Cai, Dongsheng Zhu, Qiuping Xiang
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Pyrrolidinone Derivatives as NIK Inhibitors for Treating Inflammatory and Autoimmune Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-14 Ram W. Sabnis
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Suppressive Effects of Neuromedin U Receptor 2-Selective Peptide Agonists on Appetite and Prolactin Secretion in Mice ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-14 Asuka Nomoto, Yui Suzuki, Katsuya Morito, Kazuki Nagasawa, Kentaro Takayama
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Innovations in Pharmacology: Enhancing Bioavailability and Efficacy through Novel Compositions ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Robert B. Kargbo
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Pioneering Methods in Brain Optimization and Mental Health Treatment ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Robert B. Kargbo
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Novel Heterocyclic Compounds for Treating Huntington’s Disease ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Ram W. Sabnis, Anika R. Sabnis
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Novel AT2R Antagonists for Treating Chronic Pain ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Ram W. Sabnis
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AI in Pharma: Transforming Drug Discovery and Strategic Management with MYC-Modulating Compounds and BET Protein Inhibitors ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-13 Robert B. Kargbo
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Advancements in Predictive Medicine: NLRP3 Inflammasome Inhibitors and AI-Driven Predictive Health Analytics ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-12 Robert B. Kargbo
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Selective Recognition of c-KIT 1 G-Quadruplex by Structural Tuning of Heteroaromatic Scaffolds and Side Chains ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-12 Khushnood Fatma, Prasanth Thumpati, Deepanjan Panda, Ravichandiran Velayutham, Jyotirmayee Dash
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Synthesis and Biophysical Characterization of Fingolimod Derivatives as Cardiac Troponin Antagonists ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-07 Laszlo Kondacs, Priyanka Parijat, Alexander J. A. Cobb, Thomas Kampourakis
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Discovery of Alternative Binding Poses through Fragment-Based Identification of DHODH Inhibitors ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-07 Lindsey G. DeRatt, E. Christine Pietsch, Justin S. Cisar, Edgar Jacoby, Faraz Kazmi, Rosalie Matico, Paul Shaffer, Alexandra Tanner, Weixue Wang, Ricardo Attar, James P. Edwards, Scott D. Kuduk
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TYK2 Inhibitors for Treating Autoimmune and Inflammatory Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-06 Ram W. Sabnis
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Improving Activity of New Arylurea Agents against Multidrug-Resistant and Biofilm-Producing Staphylococcus epidermidis ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-02-05 Vittorio Canale, Iwona Skiba-Kurek, Karolina Klesiewicz, Monika Papież, Marlena Ropek, Bartosz Pomierny, Kamil Piska, Paulina Koczurkiewicz-Adamczyk, Joanna Empel, Elżbieta Karczewska, Paweł Zajdel
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Novel Tetrahydropyrido[3,4-d]pyrimidines as HPK1 Inhibitors for Treating Cancer, Inflammatory, and Autoimmune Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-31 Ram W. Sabnis
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Redefining Neurodegenerative Treatment: Synergy of KEAP1, PROTACs, and Inflammatory Modulators ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-29 Robert B. Kargbo
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Discovery and Characterization of Active CBP/EP300 Degraders Targeting the HAT Domain ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-26 Iván Cheng-Sánchez, Katherine A. Gosselé, Leonardo Palaferri, Mariia S. Kirillova, Cristina Nevado
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Novel Fused Triazole Compounds as RIPK1 Inhibitors for Treating Neurodegenerative, Autoimmune, and Inflammatory Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-26 Ram W. Sabnis
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Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP) ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-25 Chenmao Zhou, Xinyue Hao, Zhengyang Chen, Runze Zhang, Qian Zhou, Zisheng Fan, Mingyue Zheng, Hui Hou, Sulin Zhang, Hao Guo
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Innovations in Precision Oncology: Biomarker-Driven Approaches for Enhanced Cancer Therapy ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-25 Robert B. Kargbo
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Design of Novel 18F-Labeled Amino Acid Tracers Using Sulfur 18F-Fluoride Exchange Click Chemistry ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-24 Yong Huang, Hualong Chen, Lu Zhang, Yi Xie, Chengze Li, Ziyue Yu, Zeng Jiang, Wei Zheng, Zhongjing Li, Xuan Ge, Ying Liang, Zehui Wu
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Nicotinamide Phosphoribosyltransferase Positive Allosteric Modulators Attenuate Neuronal Oxidative Stress ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-24 Jesse Gordon-Blake, Kiira Ratia, Victoria Weidig, Ganga Reddy Velma, Martha Ackerman-Berrier, Christopher Penton, Soumya Reddy Musku, Erick T.M. Alves, Tom Driver, Leon Tai, Gregory R. J. Thatcher
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Neuropharmacological Advances: Harnessing 5-HT2A Receptor Modulators and Psychoplastogens ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-23 Robert B. Kargbo
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Innovative Therapeutic Strategies in TYK2-Targeted Treatments: From Cancer to Autoimmune Disorders ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-23 Robert B. Kargbo
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Novel Heterocyclic PAD4 Inhibitors for Treating Multiple Diseases ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-23 Ram W. Sabnis
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Structure–ATPase Activity Relationship of Rhodamine Derivatives as Potent Inhibitors of P-Glycoprotein CmABCB1 ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-19 Sorachi Miwa, Hiroshi Takikawa, Rina Takeuchi, Ryo Mizunuma, Keita Matsuoka, Haruo Ogawa, Hiroaki Kato, Kiyosei Takasu
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Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-19 Navoda Jayakodiarachchi, Mallory A. Maurer, Daniel C. Schultz, Cayden J. Dodd, Analisa Thompson Gray, Hyekyung P. Cho, Olivier Boutaud, Carrie K. Jones, Craig W. Lindsley, Aaron M. Bender
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Cannabidiol-Based Prodrugs: Synthesis and Bioevaluation ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-16 Pankaj Singh Cham, Pankul Kotwal, Kuhu Sharma, Sumit Dhiman, Lakhvinder Singh, Varun Pratap Singh, Ajay Kumar, Utpal Nandi, Parvinder Pal Singh
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Synthesis and Structural Optimization of ATG4B Inhibitors for the Attenuation of Autophagy in Glioblastoma ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-16 Dalton R. Kim, Meghan J. Orr, Xiaozhou Yu, Hasan H. Munshi, Austin Wang, Claire Trudeau, Ada J. Kwong, Shi-Yuan Cheng, Karl A. Scheidt
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In This Issue ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-11 Naomi S. Rajapaksa
This article has not yet been cited by other publications.
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Novel Pyrrolo-pyrazol-one Ligands of Alpha-Synuclein for Diagnosis of Parkinson’s Disease ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-12 Gerard Rosse
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Enhanced Inhibition of Cancer Cell Migration by a Planar Catechin Analog ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-10 Hiromu Ito, Yoshimi Shoji, Ken-ichiro Matsumoto, Kiyoshi Fukuhara, Ikuo Nakanishi
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Development of a GC-376 Based Peptidomimetic PROTAC as a Degrader of 3-Chymotrypsin-like Protease of SARS-CoV-2 ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-10 Deborah Grifagni, Elena Lenci, Alessia De Santis, Andrea Orsetti, Carlo Giorgio Barracchia, Filomena Tedesco, Raffaele Bellini Puglielli, Francesca Lucarelli, Angela Lauriola, Michael Assfalg, Francesca Cantini, Vito Calderone, Daniele Guardavaccaro, Andrea Trabocchi, Mariapina D’Onofrio, Simone Ciofi-Baffoni
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Total Synthesis as Training for Medicinal Chemistry ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-10 Lewis D. Pennington
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Lysophosphatidylcholines Enriched with cis and trans Palmitoleic Acid Regulate Insulin Secretion via GPR119 Receptor ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-09 Marcin Szustak, Eliza Korkus, Rafal Madaj, Arkadiusz Chworos, Grzegorz Dąbrowski, Sylwester Czaplicki, Erfan Tabandeh, Gabriela Maciejewska, Maria Koziołkiewicz, Iwona Konopka, Anna Gliszczyńska, Edyta Gendaszewska-Darmach
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The Bis(1,2,3,4-tetrahydroisoquinoline) Alkaloids Cepharanthine and Berbamine Are Ligands of SK Channels ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-09 Romain Vitello, Hossein Taouba, Marine Derand, Jean-François Liégeois
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Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-09 Liqi He, Meng Yao Zhang, Matthew Cox, Qian Zhang, Andrew F. Donnell, Yong Zhang, Christine Tarby, Patrice Gill, Murugaiah A. M. Subbaiah, Thangeswaran Ramar, Maheswara Reddy, Vijaya Puttapaka, Yi-Xin Li, Prasanna Sivaprakasam, David Critton, Dawn Mulligan, Chunshan Xie, Radha Ramakrishnan, Jignesh Nagar, Shailesh Dudhgaonkar, Anwar Murtaza, Martins S. Oderinde, Gary L. Schieven, Arvind Mathur, Ashvinikumar
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Development of Novel Membrane Disrupting Lipoguanidine Compounds Sensitizing Gram-Negative Bacteria to Antibiotics ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-09 Seong-Heun Kim, Charlotte K. Hind, Guilherme F. S. Fernandes, Jingyue Wu, Dorothy Semenya, Melanie Clifford, Caleb Marsh, Silvia Anselmi, A. James Mason, Kenneth D. Bruce, J. Mark Sutton, Daniele Castagnolo
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Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-08 Yam B. Poudel, Liqi He, Matthew Cox, Qian Zhang, Walter L. Johnson, Qiang Cong, Heng Cheng, Naidu S. Chowdari, Christine Tarby, Andrew F. Donnell, Matthais Broekema, Daniel P. O’Malley, Yong Zhang, Murugaiah A. M. Subbaiah, Boda Vijay Kumar, Lakshumanan Subramani, Bei Wang, Yi-Xin Li, Prasanna Sivaprakasam, David Critton, Dawn Mulligan, Bhupindar Sandhu, Chunshan Xie, Radha Ramakrishnan, Jignesh Nagar
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Low-Barrier Hydrogen Bond Determines Target-Binding Affinity and Specificity of the Antitubercular Drug Bedaquiline ACS Med. Chem. Lett. (IF 4.2) Pub Date : 2024-01-08 Joanna Słabońska, Subrahmanyam Sappati, Antoni Marciniak, Jacek Czub