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A novel BODIPY-based theranostic agent for in vivo fluorescence imaging of cerebral Aβ and ameliorating Aβ-associated disorders in Alzheimer's disease transgenic mice RSC Med. Chem. (IF 4.1) Pub Date : 2024-03-15 Jingjing Zhang, Wenming Ren, Xiaohui Liu, Jingjing Chen, Yuteng Zeng, Huaijiang Xiang, Youhong Hu, Haiyan Zhang
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Aptamer AS411 interacts with the KRAS promoter/hnRNP A1 complex and shows increased potency against drug-resistant lung cancer RSC Med. Chem. (IF 4.1) Pub Date : 2024-03-04 Yuejie Zhu, Xiang Li, Qi Zhang, Xiantao Yang, Xudong Sun, Yi Pan, Xia Yuan, Yuan Ma, Bo Xu, Zhenjun Yang
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Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex RSC Med. Chem. (IF 4.1) Pub Date : 2024-03-05 Aliakbar Khalili Yazdi, Sumera Perveen, Cheng Dong, Xiaosheng Song, Aiping Dong, Magdalena M. Szewczyk, Matthew F. Calabrese, Agustin Casimiro-Garcia, Subramanyam Chakrapani, Matthew S. Dowling, Emel Ficici, Jisun Lee, Justin I. Montgomery, Thomas N. O'Connell, Grzegorz J. Skrzypek, Tuan P. Tran, Matthew D. Troutman, Feng Wang, Jennifer A. Young, Jinrong Min, Dalia Barsyte-Lovejoy, Peter J. Brown,
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Progress in small-molecule inhibitors targeting PD-L1 RSC Med. Chem. (IF 4.1) Pub Date : 2024-03-04 Jindan Xu, Yuanfang Kong, Pengbo Zhu, Mingyan Du, Xuan Liang, Yan Tong, Xiaofei Li, Chunhong Dong
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Synthesis and structure–activity relationship of novel thiazole aminoguanidines against MRSA and Escherichia coli RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-29 Ping Yang, Hui-Zhong Liu, Ying-Si Wang, Hong Qi, Ling-Ling Wang, Bei-Bei Wang, Xiao-Bao Xie
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The medicinal chemistry evolution of antibody–drug conjugates RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-28 Adrian D. Hobson
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Design, synthesis, and evaluation of novel ferrostatin derivatives for the prevention of HG-induced VEC ferroptosis RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-28 Xin-Xin Wang, Run-Jie Wang, Hua-Long Ji, Xiao-Yu Liu, Nai-Yu Zhang, Kai-Ming Wang, Kai Chen, Ping-Ping Liu, Ning Meng, Cheng-Shi Jiang
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Nitrogen-containing andrographolide derivatives with multidrug resistance reversal effects in cancer cells RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-26 Joana R. L. Ribeiro, Nikoletta Szemerédi, Bruno M. F. Gonçalves, Gabriella Spengler, Carlos A. M. Afonso, Maria-José U. Ferreira
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Correction: Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-22 Adrian D. Hobson, Haizhong Zhu, Wei Qiu, Russell A. Judge, Kenton Longenecker
Correction for ‘Minimising the payload solvent exposed hydrophobic surface area optimises the antibody–drug conjugate properties’ by Adrian D. Hobson et al., RSC Med. Chem., 2024, https://doi.org/10.1039/d3md00540b.
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Unusual Ni⋯Ni interaction in Ni(II) complexes as potential inhibitors for the development of new anti-SARS-CoV-2 Omicron drugs RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-20 Simranjeet Singh, Mukesh Choudhary
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Synthesis and bioactivity of psilocybin analogues containing a stable carbon–phosphorus bond RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-21 Marthe Vandevelde, Andreas Simoens, Bavo Vandekerckhove, Christian Stevens
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1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-21 Robin van der Straat, Rosalie Draijer, Ewa Surmiak, Roberto Butera, Lennart Land, Katarzyna Magiera-Mularz, Bogdan Musielak, Jacek Plewka, Tad A. Holak, Alexander Dömling
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Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-20 Mihaela-Liliana Ţînţaş, Ludovic Peauger, Anaïs Barré, Cyril Papamicaël, Thierry Besson, Jana Sopkovà-de Oliveira Santos, Vincent Gembus, Vincent Levacher
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Design, synthesis, in vitro and in silico evaluation of indole-based tetrazole derivatives as putative anti-breast cancer agents RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-19 Kamalpreet Kaur, Harkomal Verma, Prabhakar Gangwar, Monisha Dhiman, Vikas Jaitak
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Application of tobramycin benzyl ether as an antibiotic adjuvant capable of sensitizing multidrug-resistant Gram-negative bacteria to rifampicin RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-16 Danzel Marie Ramirez, Shiv Dhiman, Ayan Mukherjee, Ruwani Wimalasekara, Frank Schweizer
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In vitro biological evaluation and in silico studies of linear diarylheptanoids from Curcuma aromatica Salisb. as urease inhibitors RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-16 Tho Huu Le, Dung Ngoc Phuong Ho, Hai Xuan Nguyen, Truong Nhat Van Do, Mai Thanh Thi Nguyen, Lam K. Huynh, Nhan Trung Nguyen
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AiZynth impact on medicinal chemistry practice at AstraZeneca RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-16 Jason D. Shields, Rachel Howells, Gillian Lamont, Yin Leilei, Andrew Madin, Christopher E. Reimann, Hadi Rezaei, Tristan Reuillon, Bryony Smith, Clare Thomson, Yuting Zheng, Robert E. Ziegler
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Deconvoluting low yield from weak potency in direct-to-biology workflows with machine learning RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-15 William McCorkindale, Mihajlo Filep, Nir London, Alpha A. Lee, Emma King-Smith
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Design, synthesis and biological evaluation of rhein–piperazine–furanone hybrids as potential anticancer agents RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-13 Yu He, Si-Si Zhang, Meng-Xue Wei
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Correction: Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-12 Lakshmi Goswami, Lovely Gupta, Sayantan Paul, Maansi Vermani, Pooja Vijayaraghavan, Asish K. Bhattacharya
Correction for ‘Design and synthesis of eugenol/isoeugenol glycoconjugates and other analogues as antifungal agents against Aspergillus fumigatus’ by Lakshmi Goswami et al., RSC Med. Chem., 2022, 13, 955–962, https://doi.org/10.1039/D2MD00138A.
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Stereoselective synthesis and antiproliferative activity of allo-gibberic acid-based 1,3-aminoalcohol regioisomers RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-12 Zein Alabdeen Khdar, Tam Minh Le, Zsuzsanna Schelz, István Zupkó, Zsolt Szakonyi
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Design, quality and validation of the EU-OPENSCREEN fragment library poised to a high-throughput screening collection RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-12 Xavier Jalencas, Hannes Berg, Ludvik Olai Espeland, Sridhar Sreeramulu, Franziska Kinnen, Christian Richter, Charis Georgiou, Vladyslav Yadrykhinsky, Edgar Specker, Kristaps Jaudzems, Tanja Miletić, Robert Harmel, Phil Gribbon, Harald Schwalbe, Ruth Brenk, Aigars Jirgensons, Andrea Zaliani, Jordi Mestres
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Discovery of a new pyrido[2,3-d]pyridazine-2,8-dione derivative as a potential anti-inflammatory agent through COX-1/COX-2 dual inhibition RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-08 Fernanda A. Rosa, Davana S. Gonçalves, Karlos E. Pianoski, Michael J. V. da Silva, Franciele Q. Ames, Rafael P. Aguiar, Hélito Volpato, Danielle Lazarin-Bidóia, Celso V. Nakamura, Ciomar A. Bersani-Amado
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Design and synthesis of novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-06 Norhan A. Abdelrahman, Ahmed A. Al-Karmalawy, Maiy Y. Jaballah, Galal Yahya, Marwa Sharaky, Khaled A. M. Abouzid
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Design, synthesis and biological evaluation of novel morpholinopyrimidine-5-carbonitrile derivatives as dual PI3K/mTOR inhibitors RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-02 Ghada S. Rady, Moshira A. El Deeb, Marwa T. M. Sarg, Azza T. Taher, Amira A. Helwa
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Glucosamine substituted sulfonylureas: IRS–PI3K–PKC–AKT–GLUT4 insulin signalling pathway intriguing agent RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-01 Ghadeer A. R. Y. Suaifan, Bayan Alkhawaja, Mayadah B. Shehadeh, Mridula Sharmaa, Chan Hor Kuan, Patrick Nwabueze Okechukwu
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Reinvestigation of diphenylmethylpiperazine analogues of pyrazine as new class of Plasmodial cysteine protease inhibitors for the treatment of malaria RSC Med. Chem. (IF 4.1) Pub Date : 2024-02-01 Hari Madhav, G. Srinivas Reddy, Zeba Rizvi, Ehtesham Jameel, Tarosh S. Patel, Abdur Rahman, Vikas Yadav, Sadaf Fatima, Fatima Heyat, Kavita Pal, Amisha Minju-OP, Naidu Subbarao, Souvik Bhattacharjee, Bharat C. Dixit, Puran Singh Sijwali, Nasimul Hoda
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Inhibition of N-type calcium channels by phenoxyaniline and sulfonamide analogues RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-31 Anjie S. Bispat, Fernanda C. Cardoso, Md. Mahadhi Hasan, Yashad Dongol, Ricki Wilcox, Richard J. Lewis, Peter J. Duggan, Kellie L. Tuck
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A concept of dual-responsive prodrugs based on oligomerization-controlled reactivity of ester groups: an improvement of cancer cells versus neutrophils selectivity of camptothecin RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-31 Insa Klemt, Viktor Reshetnikov, Subrata Dutta, Galyna Bila, Rostyslav Bilyy, Itziar Cossío Cuartero, Andrés Hidalgo, Adrian Wünsche, Maximilian Böhm, Marit Wondrak, Leoni A. Kunz-Schughart, Rainer Tietze, Frank Beierlein, Petra Imhof, Sabrina Gensberger-Reigl, Monika Pischetsrieder, Marlies Körber, Tina Jost, Andriy Mokhir
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Correction: A high-throughput effector screen identifies a novel small molecule scaffold for inhibition of ten-eleven translocation dioxygenase 2 RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-29 Shubhendu Palei, Jörn Weisner, Melina Vogt, Rajesh Gontla, Benjamin Buchmuller, Christiane Ehrt, Tobias Grabe, Silke Kleinbölting, Matthias Müller, Guido H. Clever, Daniel Rauh, Daniel Summerer
Correction for ‘A high-throughput effector screen identifies a novel small molecule scaffold for inhibition of ten-eleven translocation dioxygenase 2’ by Shubhendu Palei et al., RSC Med. Chem., 2022, 13, 1540–1548, https://doi.org/10.1039/D2MD00186A.
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Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-30 Lin Tang, Minxiong Li, Changlin Bai, Xuejin Feng, Haiyang Hu, Yufen Yao, Baiqing Li, Hongwei Li, Guohong Qin, Ning Xi, Genpin Lv, Lei Zhang
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Screening of efficient salicylaldoxime reactivators for DFP and paraoxon-inhibited acetylcholinesterase RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-30 Zhao Wei, Dongxu Zhang, Xueying Liu, Huifang Nie, Qin Ouyang, Xinlei Zhang, Zhibing Zheng
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Molecular editing of NSC-666719 enabling discovery of benzodithiazinedioxide-guanidines as anticancer agents RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-30 Vajja Krishna Rao, Subarno Paul, Mitchell Gulkis, Zhihang Shen, Haritha Nair, Amandeep Singh, Chenglong Li, Arun K. Sharma, Melike Çağlayan, Chinmay Das, Biswajit Das, Chanakya N. Kundu, Satya Narayan, Sankar K. Guchhait
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Indole-containing pharmaceuticals: targets, pharmacological activities, and SAR studies RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-30 Wei Zeng, Chi Han, Sarah Mohammed, Shanshan Li, Yixuan Song, Fengxia Sun, Yunfei Du
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Cytochrome bd oxidase: an emerging anti-tubercular drug target RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-27 Pallavi Saha, Samarpita Das, Harish K. Indurthi, Rohit Kumar, Arnab Roy, Nitin Pal Kalia, Deepak K. Sharma
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N-Arylsulfonamide-based adenosine analogues to target RNA cap N7-methyltransferase nsp14 of SARS-CoV-2 RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-26 Rostom Ahmed-Belkacem, Joris Troussier, Adrien Delpal, Bruno Canard, Jean-Jacques Vasseur, Etienne Decroly, Françoise Debart
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Identification of novel phenylalanine derivatives bearing a hydroxamic acid moiety as potent quorum sensing inhibitors RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-23 Truong Thanh Tung, Nguyen Quoc Thang, Nguyen Cao Huy, Pham Bao Phuong, Dinh Ngoc Minh, Nguyen Hai Nam, John Nielsen
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Consensus screening for a challenging target: the quest for P-glycoprotein inhibitors RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-22 Paolo Governa, Marco Biagi, Fabrizio Manetti, Stefano Forli
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Development of Hsp90 C-terminal inhibitors with noviomimetics that manifest anti-proliferative activities RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-18 Eva Amatya, Chitra Subramanian, Mark S. Cohen, Brian S. J. Blagg
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Trifluoroacetic acid-mediated synthesis of xanthene constructs and their extensive anti-tuberculosis evaluation RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-12 Bisma Teli, Mohamad Mosa Mubarak, Zahoor Ahmad, Bilal A. Bhat
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Design, synthesis, and antiproliferative evaluation of novel dehydroabietic acid-1,2,3-triazole-oxazolidinone hybrids RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-11 Yaju Wu, Lin Huang, Xianli Ma, Xiaoqun Zhou, Qian Li, Fangyao Li
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Small molecules modulating RNA splicing: a review of targets and future perspectives RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-11 Léa Bouton, Agathe Ecoutin, Florian Malard, Sébastien Campagne
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Emerging potential approaches in alkaline phosphatase (ALP) activatable cancer theranostics RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-10 Kartikay Tyagi, V. Venkatesh
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Small molecule WDR5 inhibitors down-regulate lncRNA expression RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-10 Jen-Yao Chang, Cora Neugebauer, Anne Mues genannt Koers, Peter 't Hart
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Minimising the payload solvent exposed hydrophobic surface area optimises the antibody-drug conjugate properties RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-09 Adrian D. Hobson, Haizhong Zhu, Wei Qiu, Russell A. Judge, Kenton Longenecker
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Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-09 Yingpeng Liu, Radosław P. Nowak, Jianwei Che, Katherine A. Donovan, Fidel Huerta, Hu Liu, Rebecca J. Metivier, Eric S. Fischer, Lyn H. Jones
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PDE-stable 2′3′-cGAMP analogues, containing 5′-S-phosphorothioester linkage, as STING agonists RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-09 Simpa K. Yeboah, Herman O. Sintim
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Discovery of novel positive allosteric modulators targeting GluN1/2A NMDARs as anti-stroke therapeutic agents RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-04 Hongyu Zhu, Xin Chen, Lu Zhang, Xuequan Liu, Ji Chen, Han-Ting Zhang, Mingxin Dong
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Recent advances of tryptanthrin and its derivatives as potential anticancer agents RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-04 Xiaofeng Zhou
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Design, synthesis and biological evaluation of novel pyrimidine derivatives as bone anabolic agents promoting osteogenesis via the BMP2/SMAD1 signaling pathway RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-04 Sumit K. Rastogi, Sonu Khanka, Santosh Kumar, Amardeep Lakra, Rajat Rathur, Kriti Sharma, Amol Chhatrapati Bisen, Rabi Sankar Bhatta, Ravindra Kumar, Divya Singh, Arun K. Sinha
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Carbopol 940-based hydrogels loading synergistic combination of quercetin and luteolin from the herb Euphorbia humifusa to promote Staphylococcus aureus infected wound healing RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-03 Xiying Wu, Hao-Wei Chen, Ze-Yu Zhao, Lisha Li, Chi Song, Juan Xiong, Guo-Xun Yang, Quangang Zhu, Jin-Feng Hu
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Design, synthesis, and cytotoxicity of ibuprofen-appended benzoxazole analogues against human breast adenocarcinoma RSC Med. Chem. (IF 4.1) Pub Date : 2024-01-02 Vishnu Thumma, Veerabhadraiah Mallikanti, Raghavender Matta, Ravinder Dharavath, Pochampally Jalapathi
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Formulation of a fast-disintegrating drug delivery system from cyclodextrin/naproxen inclusion complex nanofibrous films RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-21 Asli Celebioglu, Kareena Dash, Mahmoud Aboelkheir, Mehmet E. Kilic, Engin Durgun, Tamer Uyar
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Beyond inhibition against the PD-1/PD-L1 pathway: development of PD-L1 inhibitors targeting internalization and degradation of PD-L1 RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-21 Jiazheng Guo, Fengyi Yu, Kuojun Zhang, Sheng Jiang, Xiangyu Zhang, Tianyu Wang
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Highly potent and selective phosphatidylinositol 4-kinase IIIβ inhibitors as broad-spectrum anti-rhinoviral agents RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-21 Avinash G Vishakantegowda, Dasom Hwang, Prashant Chakrasali, Eunhye Jung, Joo-Youn Lee, Jin Soo Shin, Young-Sik Jung
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The allure of targets for novel drugs RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-13 Colin J. Suckling
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1-Benzylindoles as inhibitors of cytosolic phospholipase A2α: synthesis, biological activity, aqueous solubility, and cell permeability RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-13 Imke Meyer zu Vilsendorf, Judith Einerhand, Dennis Mulac, Klaus Langer, Matthias Lehr
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Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-12 Baku Acharya, Debasmita Saha, Daniel Armstrong, Baha'a Jabali, Maha Hanafi, Alan Herrera-Rueda, Naga Rajiv Lakkaniga, Brendan Frett
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Role of heterocycles in inhibition of VEGFR-2 – a recent update (2019–2022) RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-12 Atukuri Dorababu
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Discovery of new dibenzodiazepine derivatives as antibacterials against intracellular bacteria RSC Med. Chem. (IF 4.1) Pub Date : 2023-12-11 Ling-Han Chen, Man-Yi Lin, Hsueh-Chun Lin, Fan-Wei Yang, Hsiao-Wei Liao, Chung-Wai Shiau, Hao-Chieh Chiu, Jung-Chen Su