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Discovery of dual inhibitors of topoisomerase I and Cyclooxygenase-2 for colon cancer therapy Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-23 Xiaoling Hu, Junfang Li, Honghua Zhang, Quanwei Yu, Yuying Wang, Xuelin Li, Lin Long, Weifan Jiang, Zhen Wang
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Membrane acting Povarov-Doebner derived compounds potently disperse preformed multidrug resistant Gram-positive bacterial biofilms Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-23 Neetu Dayal, Kenneth I. Onyedibe, Whitney M. Gribble, Herman O. Sintim
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Synthesis and anti-trypanosomal evaluation of novel N-branched acyclic nucleoside phosphonates bearing 7-aryl-7-deazapurine nucleobase Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-23 Karolína Vaňková, Eva Doleželová, Eva Tloušťová, Dana Hocková, Alena Zíková, Zlatko Janeba
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Influence of chain length on the anticancer activity of the antimicrobial peptide CAMEL with fatty acid modification Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-23 Ling Ma, Sujie Huang, Huan Xie, Panpan Ma, Bo Jia, Yufan Yao, Yuxuan Gao, Wenyuan Li, Jingjing Song, Wei Zhang
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Computational method for the systematic alignment of analogue series with structure-activity relationship transfer potential across different targets Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-23 Atsushi Yoshimori, Jürgen Bajorath
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Identification of (S)-1-(2-(2,4-difluorophenyl)-4-oxothiazolidin-3-yl)-3-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)urea as a potential anti-colorectal cancer agent Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-22 Baohui Qi, Fei Wang, Huan He, Mengmeng Fan, Liping Hu, Li Xiong, Guowei Gong, Shengmin Shi, Xiaomeng Song
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Log P analyzation-based discovery of GSH activated biotin-tagged fluorescence probe for selective colorectal cancer imaging Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-22 Jialiang Lu, Qianqian Wang, Zhaojun Wang, Jinguo Liu, Yu Guo, Chenghao Pan, Xin Li, Jinxin Che, Zheng Shi, Shuo Zhang
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Design, synthesis and biological evaluation of biphenyl-benzamides as potent FtsZ inhibitors Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-21 Jingjing Deng, Tao Zhang, Baiqing Li, Mingyuan Xu, Yuanze Wang
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Discovery of pomalidomide-based PROTACs for selective degradation of histone deacetylase 8 Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-21 Zhiqiang Sun, Bulian Deng, Zichao Yang, Ruiyao Mai, Junli Huang, Zeli Ma, Ting Chen, Jianjun Chen
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HIV nucleoside reverse transcriptase inhibitors Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-20 Franck Amblard, Dharmeshkumar Patel, Eleftherios Michailidis, Steven J. Coats, Mahesh Kasthuri, Nicolas Biteau, Zahira Tber, Maryam Ehteshami, Raymond F. Schinazi
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Dual-target Janus kinase (JAK) inhibitors: Comprehensive review on the JAK-based strategies for treating solid or hematological malignancies and immune-related diseases Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-18 Pei Shen, Yezhi Wang, Xiangxiang Jia, Pengfei Xu, Lian Qin, Xi Feng, Zhiyu Li, Zhixia Qiu
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Synthesis and biological evaluation of tyrosine derivatives as peripheral 5HT2A receptor antagonists for nonalcoholic fatty liver disease Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-15 Minhee Kim, Wonil Choi, Jihyeon Yoon, Byung-kwan Jeong, Suvarna H. Pagire, Haushabhau S. Pagire, Jungsun Park, Jung Eun Nam, Chang Joo Oh, Jae-Han Jeon, Seong Soon Kim, Byung Hoi Lee, Jin Sook Song, Myung Ae Bae, In-Kyu Lee, Hail Kim, Jin Hee Ahn
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Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-17 Jessica Plescia, Damien Hédou, Maud Eva Pousse, Anne Labarre, Caroline Dufresne, Anthony Mittermaier, Nicolas Moitessier
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Designing quinoline-isoniazid hybrids as potent anti-tubercular agents inhibiting mycolic acid biosynthesis Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-17 Matthéo Alcaraz, Bharvi Sharma, Françoise Roquet-Banères, Cyril Conde, Thierry Cochard, Franck Biet, Vipan Kumar, Laurent Kremer
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Recent advances in the development of EGFR degraders: PROTACs and LYTACs Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-16 Dawei Hong, Bizhong Zhou, Bei Zhang, Hao Ren, Liquan Zhu, Guowan Zheng, Minghua Ge, Jingyan Ge
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Bis-chalcone polyphenols with potential preventive and therapeutic effects on PD: Design, synthesis and in vitro disaggregation activity against α-synuclein oligomers and fibrils Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-16 Bing Jiang, Feng Han, Ming-Huan Lü, Zhen-Ping Wang, Wei Liu, Yun-Xiao Zhang, Ji Xu, Rui-Jun Li
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Design, synthesis and bioactivity evaluation of favorable evodiamine derivative scaffold for developing cancer therapy Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-15 Ziyi Liang, Yuqing Wang, Honghua Zhang, Jiedan Deng, Fang Lei, Junfang Li, Tao Shi, Shuzhi Wang, Ranhui Li, Zhen Wang
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Cancer multidrug-resistance reversal by ABCB1 inhibition: A recent update Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-17 Kritika Engle, Gautam Kumar
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Design and development of a novel series of oral bivalent BET inhibitors with potent anticancer activities Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-11 Menglan Luo, Qian Wu, Yueyue Yang, Lin Sun, Xiajuan Huan, Changqing Tian, Bing Xiong, Zehong Miao, Yingqing Wang, Danqi Chen
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Synthesis and evaluation of imidazo[1,2-a]pyrazine derivatives as small molecule Gαq/11 inhibitors against uveal melanoma Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-11 Jun-Jie Deng, Lu Liu, Yang Ge, Zhendong Song, Jie Huang, Guangjin Fan, Xiao-Feng Xiong
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Discovery of 1,3,4-oxadiazole derivatives containing a bisamide moiety as a novel class of potential cardioprotective agents Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-11 Fei-Fei Yang, Jin-Zhu Zhou, Xue-Li Xu, Ting Hu, Jian-Quan Liu, Ya-Xi Wu, Bo Wei, Li-Ying Ma
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Designing and development of phthalimides as potent anti-tubulin hybrid molecules against malaria Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-15 Vigyasa Singh, Rahul Singh Hada, Ravi Jain, Manu Vashistha, Geeta Kumari, Snigdha Singh, Neha Sharma, Meenakshi Bansal, Poonam, Martin Zoltner, Conor R. Caffrey, Brijesh Rathi, Shailja Singh
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Discovery of novel orexin receptor antagonists using a 1,3,5-trioxazatriquinane bearing multiple effective residues (TriMER) library Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-13 Tsuyoshi Saitoh, Mao Amezawa, Jumpei Horiuchi, Yasuyuki Nagumo, Naoshi Yamamoto, Noriki Kutsumura, Ryuichiro Ohshita, Akihisa Tokuda, Yoko Irukayama-Tomobe, Yasuhiro Ogawa, Yukiko Ishikawa, Emi Hasegawa, Takeshi Sakurai, Yasuo Uchida, Tetsu Sato, Hiroaki Gouda, Ryuji Tanimura, Masashi Yanagisawa, Hiroshi Nagase
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Discovery of dearomatized isoprenylated acylphloroglucinols with colon tumor suppressive activities in mice via inhibiting NFκB-FAT1-PDCD4 signaling activation Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-14 Na-Na Jiang, Grace Gar-Lee Yue, Peng Li, Yan-Song Ye, Adele Joyce Gomes, Frankie Hin-Fai Kwok, Julia Kin-Ming Lee, Si Gao, Clara Bik-San Lau, Gang Xu
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Dual-target inhibitors of indoleamine 2, 3 dioxygenase 1 (Ido1): A promising direction in cancer immunotherapy Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-08 Ya Zhang, Zelin Hu, Jifa Zhang, Changyu Ren, Yuxi Wang
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Identification of dihydroquinolizinone derivatives with cyclic ether moieties as new anti-HBV agents Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-08 Xiaoyu Qin, Lu Yang, Xican Ma, Bin Jiang, Shuo Wu, Apeng Wang, Shijie Xu, Wenhao Wu, Huijuan Song, Na Du, Kai Lv, Yuhuan Li, Mingliang Liu
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Discovery of a potent and selective proteolysis targeting chimera (PROTAC) degrader of NSD3 histone methyltransferase Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-13 Yaoliang Sun, Ying Zhang, Xiaoai Chen, Aisong Yu, Wenhao Du, Yuting Huang, Feifei Wu, Lei Yu, Jiayi Li, Cuiyun Wen, Hong Yang, Qiongyu Shi, Meiyu Geng, Xun Huang, Shilin Xu
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Pan- and isoform-specific inhibition of Hsp90: Design strategy and recent advances Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-07 Jing Yu, Chao Zhang, Chun Song
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Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-06 Kevin Antraygues, Mathieu Maingot, Birgit Schellhorn, Vincent Trebosc, Marc Gitzinger, Benoit Deprez, Olivier Defert, Glenn E. Dale, Marilyne Bourotte, Sergio Lociuro, Nicolas Willand
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Discovery of highly potent and selective CRBN-recruiting EGFRL858R/T790M degraders in vivo Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-06 Wenjuan Zhang, Pengyun Li, Shiyang Sun, Changkai Jia, Ning Yang, Xiaomei Zhuang, Zhibing Zheng, Song Li
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Design, synthesis and biological evaluation of novel osimertinib derivatives as reversible EGFR kinase inhibitors Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-07 Shi Ding, Ziye Gao, Ziqiang Hu, Rui Qi, Xiangshan Zheng, Xiaoyong Dong, Mingjuan Zhang, Jiwei Shen, Tian Long, Yan Zhu, Lu Tian, Wenshan Song, Ruoqing Liu, Ying Li, Jiahuan Sun, Wenwen Duan, Ju Liu, Ye Chen
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Identification of novel indole derivatives as highly potent and efficacious LSD1 inhibitors Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-10 Xiangyu Zhang, Yixiang Sun, Hailan Huang, Xinran Wang, Tianxiao Wu, Wenbo Yin, Xiaojia Li, Lin Wang, Yanting Gu, Dongmei Zhao, Maosheng Cheng
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A comprehensive review on acridone based derivatives as future anti-cancer agents and their structure activity relationships Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-10 Tanuja T. Yadav, Manikanta Murahari, G.J. Peters, Mayur YC
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Discovery of novel phenylhydrazone-based oxindole-thiolazoles as potent antibacterial agents toward Pseudomonas aeruginosa Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-09 Fen-Fen Li, Wen-Hao Zhao, Vijai Kumar Reddy Tangadanchu, Jiang-Ping Meng, Cheng-He Zhou
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Azole inhibitors of mushroom and human tyrosinases: Current advances and prospects of drug development for melanogenic dermatological disorders Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-09 Usman Ghani
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Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-03 Jie Liu, Lu Liu, Lei Zheng, Kai-Wen Feng, Hai-Tao Wang, Jiang-Ping Xu, Zhong-Zhen Zhou
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Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-03 Xiaodong Dou, Qi Sun, Guofeng Xu, Yameng Liu, Caifang Zhang, Bingding Wang, Yangbin Lu, Zheng Guo, Lingyu Su, Tongyu Huo, Xinyi Zhao, Chen Wang, Zhongtian Yu, Song Song, Liangren Zhang, Zhenming Liu, Luhua Lai, Ning Jiao
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Expansion of the S–CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-03 Xu Ling, Qing-Qing Hao, Christophe Pannecouque, Erik De Clercq, Fen-Er Chen
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A highly effective and stable butyrylcholinesterase inhibitor with multi-faceted neuroprotection and cognition improvement Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-07 Qi Li, Baichen Xiong, Yuanyuan Wang, Weiping Lyu, Shuaishuai Xing, Ying Chen, Qinghong Liao, Siyu He, Feng Feng, Wenyuan Liu, Yao Chen, Haopeng Sun
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Design, synthesis, and structure–activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-07 Yasushi Hattori, Shigemitsu Matsumoto, Shinji Morimoto, Masaki Daini, Masashi Toyofuku, Satoru Matsuda, Rina Baba, Koji Murakami, Misa Iwatani, Hideyuki Oki, Shinji Iwasaki, Kouta Matsumiya, Yusuke Tominari, Haruhide Kimura, Mitsuhiro Ito
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Design and synthesis of chromone-based monoamine oxidase B inhibitors with improved drug-like properties Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-03 Joana Reis, Carlos Fernandes, Hoda Salem, Marta Maia, Cláudia Tomé, Sofia Benfeito, José Teixeira, Paulo J. Oliveira, Eugenio Uriarte, Francesco Ortuso, Stefano Alcaro, Donatella Bagetta, Fernando Cagide, Fernanda Borges
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Estrogen receptor β-targeted hypoxia-responsive near-infrared fluorescence probes for prostate cancer study Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-02 Baohua Xie, Qiuyu Meng, Huiguang Yu, Kang Shen, Yan Cheng, Chune Dong, Hai-Bing Zhou
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Design and synthesis of a novel non peptide CN-NFATc signaling inhibitor for tumor suppression in triple negative breast cancer Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-04 Adrià Sánchez-Morales, Atilla Biçer, Vasilis Panagiotopoulos, Selma Crecente-Garcia, Cristina Benaiges, Sergi Bayod, José Luís Hernández, Félix Busqué, Minos-Timotheos Matsoukas, Mercè Pérez-Riba, Ramon Alibés
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Marine natural products and their synthetic analogs as promising antibiofilm agents for antibiotics discovery and development Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-04 Yueting Deng, Yang Liu, Juan Li, Xiao Wang, Shan He, Xiaojun Yan, Yutong Shi, Weiyan Zhang, Lijian Ding
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Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-02 Valentin Duvauchelle, Patrick Meffre, Zohra Benfodda
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Design, synthesis and anti-inflammatory evaluation of aloe-emodin derivatives as potential modulators of Akt, NF-κB and JNK signaling pathways Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-02 Hai Shang, Jing Guo, Pengtao Wang, Lingyu Li, Yu Tian, Xiaoxue Li, Zhongmei Zou
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Identification of new FK866 analogues with potent anticancer activity against pancreatic cancer Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-06-02 Jian-Fei Bai, Somi Reddy Majjigapu, Bernard Sordat, Sophie Poty, Pierre Vogel, Pilar Elías-Rodríguez, Antonio J. Moreno-Vargas, Ana T. Carmona, Irene Caffa, Moustafa Ghanem, Amr Khalifa, Fiammetta Monacelli, Michele Cea, Inmaculada Robina, Consuelo Gajate, Faustino Mollinedo, Axel Bellotti, Aimable Nahimana, Alessio Nencioni
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Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-31 Hongjin Zhai, Chunying Luo, Pu Yang, Shuo Zhang, Huanhuan Wang, Yaquan Cao, Yingxue Yang, Haoyue Liu, Xiaoyan Kong, Firas Obald Arhema Frejat, Changzhong Ren, Xiufang Shi, Chunli Wu
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Identification and anti-tumor evaluation of 3-acyl-indol-based 2,4-diarylaminopyrimidine analogues as potent ALK inhibitors capable of overcoming drug-resistant mutants Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-30 Ming Guo, Hao Wang, Jing Yang, Xinyu Wang, Jiahao Zhang, Shuyu Liu, Shangfei Wei, Nan Jiang, Xin Zhai
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Discovery of novel Thieno[2,3-d]imidazole derivatives as agonists of human STING for antitumor immunotherapy using systemic administration Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-30 Jing Niu, Hudagula Bai, Zizhou Li, Yuzhe Gao, Yan Zhang, Xiyuan Wang, Yaxi Yang, Yungen Xu, Meiyu Geng, Zuoquan Xie, Bing Zhou
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A novel series of teriflunomide derivatives as orally active inhibitors of human dihydroorotate dehydrogenase for the treatment of colorectal carcinoma Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-26 Chungen Li, Yue Zhou, Jing Xu, Xia Zhou, Zongkai Huang, Ting Zeng, Xiaowei Yang, Lei Tao, Kun Gou, Xi Zhong, Qiang Chen, Youfu Luo, Yinglan Zhao
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Design and synthesis of highly TRAIL expression HDAC inhibitors based on ONC201 to promote apoptosis of colorectal cancer Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-27 Hao Cui, Zan Hu, Kang Yang, Jingkun Huang, Yichao Wu, Quanwei Chen, Ran Wei, Penfeng Wang, Hui Wang, Hongmei Li, Yadong Chen, Tao Lu, Yuqin Yao, Yong Zhu
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A bioisosteric approach to the discovery of novel N-aryl-N′-[4-(aryloxy)cyclohexyl]squaramide-based activators of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-29 Jinsook Kwak, Min-Jung Kim, Soyeong Kim, Ga-Bin Park, Jeyun Jo, Myeonggyo Jeong, Seongeun Kang, Sungwon Moon, Seorin Bang, Hongchan An, Seonghwan Hwang, Min-Soo Kim, Jin-Wook Yoo, Hyung Ryong Moon, Woochul Chang, Ki Wung Chung, Jee-Yeong Jeong, Hwayoung Yun
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Targeted therapy and drug resistance in thyroid cancer Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-29 Yujie Zhang, Zhichao Xing, Tianyou Liu, Minghai Tang, Li Mi, Jingqiang Zhu, Wenshuang Wu, Tao Wei
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trans, trans-2-C-Aryl-3,4-dihydroxypyrrolidines as potent and selective β-glucosidase inhibitors: Pharmacological chaperones for Gaucher disease Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-29 Jun-Zhe Wang, Yuna Shimadate, Maki Kise, Atsushi Kato, Yue-Mei Jia, Yi-Xian Li, George W.J. Fleet, Chu-Yi Yu
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Novel quinoline-based derivatives: A new class of PDE4B inhibitors for adjuvant-induced arthritis Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-28 Siqi Xing, Weizheng Fan, Junhua Chen, Jiyu Du, Tongtong Liu, Shuanghong Dong, Jucheng Xia, Peipei Liu, Dexing Zou, Li Cai, Zeng Li
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Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015–2021) Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-28 Patrik Oleksak, Eugenie Nepovimova, Zofia Chrienova, Kamil Musilek, Jiri Patocka, Kamil Kuca
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Ring replacement recommender: Ring modifications for improving biological activity Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-23 Peter Ertl, Eva Altmann, Sophie Racine, Richard Lewis
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The polyamino-isoprenyl potentiator NV716 revives disused antibiotics against Gram-negative bacteria in broth, infected monocytes, or biofilms, by disturbing the barrier effect of their outer membrane Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-27 Gang Wang, Jean-Michel Brunel, Hector Rodriguez-Villalobos, Jean-Michel Bolla, Françoise Van Bambeke
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Melphalan: Recent insights on synthetic, analytical and medicinal aspects Eur. J. Med. Chem. (IF 6.514) Pub Date : 2022-05-27 Rakesh Pahwa, Jatin Chhabra, Raj Kumar, Rakesh Narang
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