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Design, synthesis, and biological evaluation of novel highly potent FXR agonists bearing piperidine scaffold Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-19 Wenxin Wang, Zongyu Cai, Zhilin Liang, Zibin Liao, Yuxia Liu, Xinqian Geng, Yuanqian Yang, Yisi Chen, Zibin Huang, Ying Yang, Zheng Li
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Discovery of Potent and Selective Factor XIa Inhibitors Incorporating Triazole-Based Benzoic Acid as Novel P2’ Fragments: Molecular Dynamics Simulations and Anticoagulant Activity Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-19 Linjun Dai, Yanqing Qiu, Qingrui Xu, Feng Yang, Boquan Ren, Xinyu Zhuang, Ruixin Li, Junhao Xing, Yan-Jun Xu, Qing Li
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α-GalCer sp2-iminoglycolipid analogs as CD1d-dependent iNKT modulators: Evaluation of their immunotherapeutic potential in murine models of asthma and autoimmune hepatitis Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-15 Alan Chuan-Ying Lai, Manuel González-Cuesta, Chieh-Hsin Ho, Po-Yu Chi, Ko-Chien Wu, Gabriel Rocha, Juan C. Muñoz-García, Jesús Angulo, José M. García Fernández, Ya-Jen Chang, Carmen Ortiz Mellet
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Impact of the hydrophilic-lipophilic balance of free-base and Zn(II) tricationic pyridiniumporphyrins and irradiation wavelength in PDT against the melanoma cell lines Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-15 Martina Mušković, Martin Lončarić, Ivana Ratkaj, Nela Malatesti
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Optimization of SHP2 Allosteric Inhibitors with Novel Tail Heterocycles and Their Potential as Antitumor Therapeutics Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-18 Chengchun Zhu, Leilei Li, Yan Yu, Xiao Wang, Ying Shi, Yiping Gao, Kai Chen, Xiaoyu Liu, Yuqian Cui, Tao Zhang, Zhiyi Yu
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Discovery of a Highly Potent, N-terminal Domain-targeting degrader of AR-FL/AR-V7 for the treatment of Prostate Cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-18 Si Ha, Chenxuan Ji, Jiaqi Yang, Maoxu Xiao, Ziyi Xu, Wei-Wei Pan, Hua Xiang, Guoshun Luo
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DNA or Not DNA —That is the Question Determining the Design of Platinum Anticancer Drugs Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-17 Suxing Jin, Chenyao Feng, Xiaoyong Wang
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Novel potent SOS1 inhibitors containing a tricyclic quinazoline scaffold: a joint view of experiments and simulations Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-17 Luolong Qing, Zhengzai Cheng, Juan Xu, Ziwei Wang, Yuanyuan Li, Mario Gauthier, Silong Zhang, Huan He
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Design, synthesis and anti-tumor evaluation of novel pyrimidine and quinazoline analogues Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-18 Ren-Jie Lin, Lin Xie, Tian-Yu Gao, Yi-Zhou Yang, Lan Huang, Kui Cheng, Zhi-Peng Chen
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Discovery of a potent PARP1 PROTAC as a chemosensitizer for the treatment of colorectal cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-17 Mingfei Wu, Yiming Jiang, Daoming Zhang, Yiquan Wu, Yuyuan Jin, Tao Liu, Xinfei Mao, Hengyuan Yu, Tengfei Xu, Yong Chen, Wenhai Huang, Jinxin Che, Bo Zhang, Tao Liu, Nengming Lin, Xiaowu Dong
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Promising Breakthroughs in Amyotrophic Lateral Sclerosis Treatment through Nanotechnology's Unexplored Frontier Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-16 Soheil Sojdeh, Moein Safarkhani, Hossein Daneshgar, Abdullah Aldhaher, Golnaz Heidari, Ehsan Nazarzadeh Zare, Siavash Iravani, Ali Zarrabi, Navid Rabiee
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Discovery of A Potent Anticancer Agent against Pancreatic Ductal Adenocarcinoma Targeting FAK with DFG-out State and JAK/Aurora Kinases Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-15 Rong-Hong Zhang, Ting Chen, Qian-Qian Xiong, Shan Wang, Guo-Qi Chen, Wen-Li Zhang, Hong-Fei Yuan, Yong-Long Zhao, Ting Liu, Yong Huang, Meng Zhou, Cheng-Li Yang, Shang-Gao Liao, Yong-Jun Li
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Discovery of novel KSP-targeting PROTACs with potent antitumor effects in Vitro and in Vivo Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-16 Deng-Gao Zhao, JieYing Liu, Zhengxi Su, Wenbo Zou, Qianwei Zhou, Ting Yin, Tan Jiyao, Yan-Yan Ma
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Synthesis, biological evaluation and mechanism study of a novel indole-pyridine chalcone derivative as antiproliferative agent against tumor cells through dual targeting tubulin and HK2 Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-16 Mengzhu Zheng, Guangyuan Liu, Yawei Han, Pengyu Qian, Mingze Wu, Ming Xiang, Yirong Zhou
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LAT1 transporter as a target for breast cancer diagnosis and therapy Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-15 Z.Y. Zhou, T. Zhu, W.L. Zheng, Z.X. Zou, Q.F. Shan, Qing Chen, Gang Wang
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Comprehensive Exploration of Isocitrate Dehydrogenase (IDH) Mutations: Tumorigenesis, Drug Discovery, and Covalent Inhibitor Advances Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-15 Conghao Gai, Hairong Zeng, Haoming Xu, Xiaoyun Chai, Yan Zou, Chunlin Zhuang, Guangbo Ge, Qingjie Zhao
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A novel androgen-independent radiotracer with dual targeting of NTSR1 and PSMA for PET/CT imaging of prostate cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-14 Qiong Wang, Zhongjing Li, Yong Huang, Chengze Li, Yiluo Li, Yi Peng, Zonghai Sheng, Ying Liang
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Nanomaterials exert biological effects by influencing the ubiquitin-proteasome system Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-15 Zhen Ai, Dan Li, Shuquan Lan, Chao Zhang
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Synthesis, evaluation and mechanism study of novel pyrazole enamides to alleviate lung injury Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-15 Guoping Zhang, Mengjie Li, Yanghui Ou, Liya Ma, Jiayu Li, Kexin Sun, Tingting Xia, Jingbo Wang, Liyan Song, Yang Liu, Ran Lin, Hongliang Yao
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Discovery and structure-activity relationship study of nicotinamide derivatives as DNA demethylase ALKBH2 inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-14 Ke Xu, Feng Li, Liang Xiong, Yinping Guo, Jian Zhang, Yuyang Wang, Shanmian Ji, Shengyong Yang, Linli Li
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Anticancer activity of salinomycin quaternary phosphonium salts Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-14 Marta Jędrzejczyk, Michał Sulik, Magdalena Mielczarek-Puta, Gwan Yong Lim, Małgorzata Podsiad, Jakub Hoser, Piotr Bednarczyk, Marta Struga, Adam Huczyński
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TRPM8 and TRPA1 Ideal Targets for Treating Cold-Induced Pain Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-13 Yiming Qi, Hao Gong, Zixian Shen, Limeng Wu, Zonghe Xu, Nuo Shi, Kexin Lin, Meng Tian, Zihua Xu, Xiang Li, Qingchun Zhao
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Identification of bioactive compounds with popular single-atom modifications: comprehensive analysis and implications for compound design Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-13 Bo Feng, Hui Yu, Xu Dong, Alejandro Díaz-Holguín, Huabin Hu
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Synthesis and evaluation of a novel BODIPY fluorescent probe targeting integrin αvβ3 for cancer diagnosis Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-13 Bin Rong, Xiaochun Dong, Weili Zhao
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Discovery of a novel, selective CK2 inhibitor class with an unusual basic scaffold Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-13 Hend Khalifa, Ahmed K. ElHady, Ting Liu, Walid A.M. Elgaher, Odile Filhol-Cochet, Claude Cochet, Ashraf H. Abadi, Mostafa M. Hamed, Mohammad Abdel-Halim, Matthias Engel
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Design, synthesis, and biological evaluation of novel pleuromutilin derivatives with methicillin-resistant Staphylococcus aureus -targeting phenol linker groups Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-13 Yunpeng Yi, Jiaming Zhang, Shuqian Lin, Haiting Wang, Guiyu Li, Shifa Yang, Ruofeng Shang, Rongling Zhang, Fei Li
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Allosteric inhibition of PTP1B by bromocatechol-chalcone derivatives Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-13 Chenxia Gao, Wenpeng Hu, Feng Xu, Yuxi Lin, Jiashu Chen, Dayong Shi, Pan Xing, Jiqiang Zhu, Xiangqian Li
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More than just DNA damage: Pt(ΙΙ)-NHC complexes derived from 4,5-diarylimidazoles augment immunogenic cell death Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-12 Lu Tang, Xingyu Chang, Jing Shi, Zhenfan Wen, Chunyang Bi, Wukun Liu
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Towards the design of ligands of the internal pocket TEADs C-terminal domain Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-12 Florine Toulotte, Mathilde Coevoet, Maxime Liberelle, Fabrice Bailly, Benjamin Zagiel, Muriel Gelin, Frédéric Allemand, Patrick Fourquet, Patricia Melnyk, Jean-François Guichou, Philippe Cotelle
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Structural insights into tryptamine psychedelics: The role of hydroxyl indole ring site in 5-HT2A receptor activation and psychedelic-like activity Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-12 Miyuan Zhang, Yuefeng Yang, Zhishuai Yang, Xin Wen, Cong Zhang, Peng Xiao, Yibo Wang, Jinpeng Sun, Hongshuang Wang, Xiaohui Wang
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Discovery of phenazine derivatives as a new class of non-classical ferroptosis inhibitors and efficacy evaluation on a mouse model of liver injury Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-12 Yunjie Wu, Lu Yang, Jing You, Chenyu Tian, Shengyong Yang, Linli Li
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Enantiomeric C-6 fluorinated swainsonine derivatives as highly selective and potent inhibitors of α-mannosidase and α-l-rhamnosidase: Design, synthesis and structure-activity relationship study Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-12 Feng-Teng Gao, Ming Zhang, Yuna Shimadate, Atsushi Kato, Yi-Xian Li, Yue-Mei Jia, Chu-Yi Yu
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Design, synthesis, and structure−activity relationship studies of triazolo-pyrimidine derivatives as WRN inhibitors for the treatment of MSI tumors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-12 Qibang Sui, Yuanyang Zhou, Manjia Li, Dan Wang, Rongrong Cui, Xiaoying Cai, Jia Liu, Xiaofeng Wang, Dan Teng, Jingyi Zhou, Hui Hou, Sulin Zhang, Mingyue Zheng
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Structure–activity relationship studies of Imidazo[1′,2′:1,6]pyrido[2,3-d]pyrimidine derivatives to develop selective FGFR inhibitors as anticancer agents for FGF19-overexpressed hepatocellular carcinoma Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-12 Jisook Kim, Seung Hyun Jung, Joo Chan Lee, Won Jeoung Kim, Jooyun Byun, Young Gil Ahn, Hyun-Ju Park
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Development of selective sigma-1 receptor ligands with antiallodynic activity: A focus on piperidine and piperazine scaffolds Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-10 Giuseppe Cosentino, Maria Dichiara, Francesca Alessandra Ambrosio, Claudia Giovanna Leotta, Giosuè Costa, Francesca Procopio, Giuliana Costanzo, Alessandro Raffa, Antonia Artacho-Cordón, M. Carmen Ruiz-Cantero, Lorella Pasquinucci, Agostino Marrazzo, Giovanni Mario Pitari, Enrique J. Cobos, Stefano Alcaro, Emanuele Amata
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Advances in the synthesis and engineering of conotoxins Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-10 Thao NT. Ho, Thanh Hoa Tran, Hoang Sinh Le, Richard J. Lewis
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Synthesis and preclinical evaluation of diarylamine derivative as Tau-PET radiotracer for Alzheimer's Disease Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-09 Tianqing Liu, Chao Ren, Wantong Guo, Xiaojun Zhang, Yuying Li, Yan Wang, Qilei Zhang, Baian Chen, Jiapei Dai, Xiao-xin Yan, Jinming Zhang, Li Huo, Mengchao Cui
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Multicomponent syntheses enable the discovery of novel quisinostat-derived chemotypes as histone deacetylase inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-08 Daniel Stopper, Susanna Buntrock, Kathrin Tan, Lais Pessanha de Carvalho, Linda Schäker-Hübner, Jana Held, Matthias U. Kassack, Finn K. Hansen
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Optimisation of a novel series of ENaC inhibitors, leading to the selection of the long-acting inhaled clinical candidate ETD001, a potential new treatment for cystic fibrosis Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-08 Henry Danahay, Martin Gosling, Roy Fox, Sarah Lilley, Holly Charlton, Jonathan D. Hargrave, Thomas B. Schofield, Duncan A. Hay, Naomi Went, Pearl McMahon, Frederic Marlin, John Scott, Julia Vile, Steve Hewison, Sarah Ellam, Samantha Brown, Juan Sabater, Guy Kennet, Sean Lightowler, Stephen P. Collingwood
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Design, synthesis, and X-ray structural studies of a series of highly potent, selective, and drug-like G protein-coupled receptor kinase 5 inhibitors Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-08 Arun K. Ghosh, Yueyi Chen, Ranjith Kumar Gadi, Amol Sonawane, Sandali Piladuwa Gamage, JohnJ.G. Tesmer
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Rational design and synthesis of novel N-benzylindole-based epalrestat analogs as selective aldose reductase inhibitors: An unexpected discovery of a new glucose-lowering agent (AK-4) acting as a mitochondrial uncoupler Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-08 Antonios Kousaxidis, Paolo Paoli, Lucia Kovacikova, Massimo Genovese, Alice Santi, Milan Stefek, Anthi Petrou, Ioannis Nicolaou
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Synthesis and pharmacodynamic evaluation of 2-aminoindole derivatives against influenza A virus in vitro/vivo Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-08 Zhongmou Zhang, Nanfang Wang, Jiejie Lu, Ying Qu, Yihui Song, Xinyu Yang, Zhanyong Wei, Qi Zhang, Piet Herdewijn, Junbiao Chang, Xiao-Na Wang, Zhenya Wang
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Next-generation cancer therapeutics: PROTACs and the role of heterocyclic warheads in targeting resistance Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-08 Ebna Azizal Omar, R. Rajesh, Pronoy Kanti Das, Rohit Pal, Gurubasavaraja Swamy Purawarga Matada, Lalmohan Maji
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Novel frontiers through nitrogen substitution at 6th, 10th and 11th position of artemisinin: Synthetic approaches and antimalarial activity Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-07 Priyanka Yadav, Varun Rawat, Shalini Kaushik Love, Ved Prakash Verma
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Discovery of novel thiosemicarbazone-acridine targeting butyrylcholinesterase with antioxidant, metal complexing and neuroprotector abilities as potential treatment of Alzheimer's disease: In vitro, in vivo, and in silico studies Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-07 Gleyton Leonel Silva Sousa, Nathalia Fonseca Nadur, Larissa de Almeida Peixoto Ferreira, Thiago da Silva Honório, Alice Simon, Lucio Mendes Cabral, Maria Luiza Móra Santos, Bruna Andrade, Emanuelle V. de Lima, Julia R. Clarke, Rosane Nora Castro, Ricardo Olímpio de Moura, Arthur Eugen Kümmerle
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Discovery of 4-(4-(3-(1-(2-(piperidin-1-yl)ethyl)-1H-benzo[d]imidazole-2-yl)isoxazol-5-yl)phenyl)morpholine as a novel c-Myc inhibitor against lung cancer in vitro and in vivo Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-07 Jian Gao, Jiacheng Yin, Shihao Li, Pingting Jia, Renjie Hong, Jiahui Chen, Xinxin Qu, Zihui Zhang, Mengting Li, Hui Zhao
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Discovery of novel fused-heterocycle-bearing diarypyrimidine derivatives as HIV-1 potent NNRTIs targeting tolerant region I for enhanced antiviral activity and resistance profile Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-07 Jiaojiao Dai, Xiangyi Jiang, Heng Gao, Boshi Huang, Erik De Clercq, Christophe Pannecouque, Shaoqing Du, Xinyong Liu, Peng Zhan
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Discovery of new fungal jumonji H3K27 demethylase inhibitors for the treatment of Cryptococcus neoformans and Candida auris infections Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-06 Xin Liu, Wang Li, Yang Liu, Xiaoqing Wang, Qiao Shi, Wanzhen Yang, Jie Tu, Yan Wang, Chunquan Sheng, Na Liu
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Discovery of novel phenyl urea SHP2 inhibitors with anti-colon cancer and potential immunomodulatory effects Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-06 Kaizhen Wang, Xiangyu Zhang, Yingxin Hu, Jiazheng Guo, Guoqing Shen, Kuojun Zhang, Sheng Jiang, Tianyu Wang
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Design and synthesis of glycofullerene derivatives as novel photosensitizer for potential application in PDT to treat cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-06 Xue Bai, Tian Yang, Xinle Shao, Bobo Jia, Huifang Hao, Faiz-Ur Rahman, Yongmin Zhang
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Design, synthesis, and cytotoxicity screening of novel pyrazolopyrimidines over renal cell carcinoma (UO-31 cells) as p38α inhibitors, and apoptotic cells inducing activities Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-05 Sara Y. Ewieda, Amr Sonousi, Aliaa M. Kamal, Mohamed K. Abdelhamid
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Discovery of pyrrolopyrimidinone derivatives as potent PKMYT1 inhibitors for the treatment of cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-05 Chao Wang, Yazhou Wang, Fanye Meng, Tingting Liu, Xiaomin Wang, Xin Cai, Man Zhang, Alex Aliper, Feng Ren, Alex Zhavoronkov, Xiao Ding
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Discovery of cloxiquine derivatives as potent HDAC inhibitors for the treatment of melanoma via activating PPARγ Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-04 Limin Yang, Ran Ding, Xiaojie Tong, Tong Shen, Shuting Jia, Xiqing Yan, Chong Zhang, Liqiang Wu
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Development of hybrid aptamers-engineered PROTACs for degrading VEGF165 in both tumor- and vascular endothelial cells Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-02 Ziting Feng, Duoli Xie, Fang Qiu, Jie Huang, Zhuqian Wang, Chao Liang
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Advance on the effects of algal carotenoids on inflammatory signaling pathways Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-01 Yudi Wang, Xinrong Geng, Song Qin, Tuanjie Che, Libo Yan, Biao Yuan, Wenjun Li
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Recent report on indoles as a privileged anti-viral scaffold in drug discovery Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-01 Asmita Singh, Charu Bhutani, Pankaj Khanna, Sangeeta Talwar, Sandeep Kumar Singh, Leena Khanna
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Tubulin/HDAC dual-target inhibitors: Insights from design strategies, SARs, and therapeutic potential Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-01 Zhen Zhang, Rui Su, Junao Liu, Keyu Chen, Chengjun Wu, Pinghua Sun, Tiemin Sun
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Design, synthesis, and evaluation of 4-(4-methyl-4H-1,2,4-triazol-3-yl)piperidine derivatives as potential glutaminyl cyclase isoenzyme inhibitors for the treatment of cancer Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-01 Qingqing Zhou, Zhenxin Wu, Feixia Qin, Pan He, Zhuoran Wang, Fangyi Zhu, Ying Gao, Wei Xiong, Chenyang Li, Haiqiang Wu
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Discovery of the first selective and potent PROTAC degrader for the pseudokinase TRIB2 Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-11-01 Chaowei Wen, Prathibha R. Gajjala, Yihan Liu, Bingzhong Chen, Mehtab S. Bal, Payal Sutaria, Qiao Yuanyuan, Yang Zheng, Yang Zhou, Jinwei Zhang, Weixue Huang, Xiaomei Ren, Zhen Wang, Ke Ding, Arul M. Chinnaiyan, Fengtao Zhou
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A novel life for antitumor combretastatins: Recent developments of hybrids, prodrugs, combination therapies, and antibody-drug conjugates Eur. J. Med. Chem. (IF 6.0) Pub Date : 2024-10-31 Marialuigia Fantacuzzi, Simone Carradori, Letizia Giampietro, Cristina Maccallini, Barbara De Filippis, Rosa Amoroso, Alessandra Ammazzalorso
更新日期：2024-11-13
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