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Design and discovery of boronic acid drugs Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-30 Jessica Plescia; Nicolas Moitessier
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Hypoxia-activated nanomedicines for effective cancer therapy Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-30 Mengjiao Zhou; Yuqi Xie; Shujun Xu; Jingqi Xin; Jin Wang; Tao Han; Richard Ting; Jie Zhang; Feifei An
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Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-26 Anna M. Schoepf; Stefan Salcher; Petra Obexer; Ronald Gust
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Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-25 Sumalee Kamchonwongpaisan; Netnapa Charoensetakul; Choladda Srisuwannaket; Supannee Taweechai; Roonglawan Ratanachak; Jarunee Vanichtanankul; Danoo Vitsupakorn; Uthai Arwon; Chawanee Thongpanchang; Bongkoch Tarnchompoo; Tirayut Vilaivan; Yongyuth Yuthavong
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Targeting RAS-RAF pathway significantly improves antitumor activity of Rigosertib-derived platinum(IV) complexes and overcomes cisplatin resistance Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-25 Zhikun Liu; Meng Wang; Hengshan Wang; Lei Fang; Shaohua Gou
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A novel class of selective CK2 inhibitors targeting its open hinge conformation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-25 Andrea Dalle Vedove; Francesca Zonta; Enrico Zanforlin; Nicola Demitri; Giovanni Ribaudo; Giulia Cazzanelli; Alberto Ongaro; Stefania Sarno; Giuseppe Zagotto; Roberto Battistutta; Maria Ruzzene; Graziano Lolli
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Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-24 Zhipei Sang; Keren Wang; Ping Bai; Anguo Wu; Jian Shi; Wenmin Liu; Gaofeng Zhu; Yiling Wang; Yu Lan; Zude Chen; Yiyang Zhao; Zhanpin Qiao; Changning Wang; Zhenghuai Tan
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In vitro and in vivo anticancer activity of tridentate thiosemicarbazone copper complexes: Unravelling an unexplored pharmacological target Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-24 Mauro Carcelli; Matteo Tegoni; Jennifer Bartoli; Cristina Marzano; Giorgio Pelosi; Marika Salvalaio; Dominga Rogolino; Valentina Gandin
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Breaking down the cell wall: Strategies for antibiotic discovery targeting bacterial transpeptidases Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-23 Stephen A. Cochrane; Christopher T. Lohans
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A potent photoreactive general anesthetic with novel binding site selectivity for GABAA receptors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-23 Abdelrahman R. Shalabi; Zhiyi Yu; Xiaojuan Zhou; Youssef Jounaidi; Hanwen Chen; Jiajia Dai; Daniel E. Kent; Hua-Jun Feng; Stuart A. Forman; Jonathan B. Cohen; Karol S. Bruzik; Keith W. Miller
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Identification of tetracyclic lactams as NMDA receptor antagonists with potential application in neurological disorders Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-23 Margarida Espadinha; Lucía Viejo; Ricardo Lopes; Clara Herrera-Arozamena; Elies Molins; Daniel J.V.A. dos Santos; Lídia Gonçalves; María Isabel Rodríguez-Franco; Cristóbal de los Ríos; Maria M.M. Santos
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Design, synthesis and biological evaluation of tetrahydroquinoline-based reversible LSD1 inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-21 Xinran Wang; Cai Zhang; Xiangyu Zhang; Jiangkun Yan; Jiming Wang; Qinwen Jiang; Liyu Zhao; Dongmei Zhao; Maosheng Cheng
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Matrix metalloproteinase-9 (MMP-9) and its inhibitors in cancer: A minireview Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-21 Subha Mondal; Nilanjan Adhikari; Suvankar Banerjee; Sk Abdul Amin; Tarun Jha
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Design, synthesis, in vitro and in silico studies of novel 4-oxoquinoline ribonucleoside derivatives as HIV-1 reverse transcriptase inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-20 Luana da S.M. Forezi; Mariana M.J. Ribeiro; Andressa Marttorelli; Juliana L. Abrantes; Carlos R. Rodrigues; Helena Carla Castro; Thiago Moreno L. Souza; Fernanda da C.S. Boechat; Alessandra M.T. de Souza; Maria Cecília B.V. de Souza
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Targeting drug delivery system for platinum(Ⅳ)-Based antitumor complexes Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-20 Yunshuang Zhong; Chunyan Jia; Xinzhong Zhang; Xiali Liao; Bo Yang; Yanwei Cong; Shaoping Pu; Chuanzhu Gao
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Optimization of 5-substituted thiazolyl ureas and 6-substituted imidazopyridines as potential HIV-1 latency reversing agents Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-20 William Nguyen; Jonathan Jacobson; Kate E. Jarman; Timothy R. Blackmore; Helene Jousset Sabroux; Sharon R. Lewin; Damian F. Purcell; Brad E. Sleebs
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Discovery of luotonin A analogues as potent fungicides and insecticides: Design, synthesis and biological evaluation inspired by natural alkaloid Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-20 Guan-Zhou Yang; Jian Zhang; Jing-Wen Peng; Zhi-Jun Zhang; Wen-Bin Zhao; Ren-Xuan Wang; Kun-Yuan Ma; Jun-Cai Li; Ying-Qian Liu; Zhong-Min Zhao; Xiao-Fei Shang
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Design, synthesis, and biological evaluation of 3-amino-2-oxazolidinone derivatives as potent quorum-sensing inhibitors of Pseudomonas aeruginosa PAO1 Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-20 Kai Jiang; Xinlin Yan; Jiahao Yu; Zijian Xiao; Hao Wu; Meihua Zhao; Yuandong Yue; Xiaoping Zhou; Junhai Xiao; Feng Lin
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Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-20 Ju Liu; Yilin Gong; Jiantao Shi; Xuechen Hao; Yang Wang; Yunpeng Zhou; Yunlei Hou; Yajing Liu; Shi Ding; Ye Chen
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Indole-based derivatives as potential antibacterial activity against methicillin-resistance Staphylococcus aureus (MRSA) Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-20 Hua-Li Qin; Jing Liu; Wan-Yin Fang; L. Ravindar; K.P. Rakesh
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Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-19 Cunbin Nie; Qifei Li; Yue Qiao; Jing Hu; Mengkang Gao; Yusui Wang; Zhenrui Qiao; Qiang Wang; Lin Yan; Hai Qian
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p62 as a therapeutic target for tumor Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-17 Mengmin Tao; Tian Liu; Qidong You; Zhengyu Jiang
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Antibacterial AZT derivative regulates metastasis of breast cancer cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-19 Sridhar Chirumarry; Nak-Kyun Soung; Junyeol Han; Eun Young Kim; Eun Kyoung Ryu; Young-Ho Lee; Song Yub Shin; Pethaiah Gunasekaran; Jeong Kyu Bang
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Discovery of new LXRβ agonists as glioblastoma inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-17 Hao Chen; Ziyang Chen; Zizhen Zhang; Yali Li; Shushu Zhang; Fuqiang Jiang; Junkang Wei; Peng Ding; Huihao Zhou; Qiong Gu; Jun Xu
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Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-17 Cindy Patinote; Nour Bou Karroum; Georges Moarbess; Natalina Cirnat; Issam Kassab; Pierre-Antoine Bonnet; Carine Deleuze-Masquéfa
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Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-16 Ying Wang; Xiaomei He; Chunshi Li; Yan Ma; Wenchi Xue; Baichun Hu; Jian Wang; Tingting Zhang; Fengjiao Zhang
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Specific stabilization of promoter G-Quadruplex DNA by 2,6-disubstituted amidoanthracene-9,10-dione based dimeric distamycin analogues and their selective cancer cell cytotoxicity Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-16 Soma Roy; Asfa Ali; Mohini Kamra; Kalappa Muniyappa; Santanu Bhattacharya
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Discovery of a novel series of imidazo[1′,2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-16 Chen Shi; Qian Wang; Xuemei Liao; Hui Ge; Guoyong Huo; Leduo Zhang; Na Chen; Xiong Zhai; Yuan Hong; Li Wang; Zhe Wang; Weijun Shi; Yu Mao; Jianxin Yu; Ying Ke; Guangxin Xia
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Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-16 Xiang Nan; Hui-Jing Li; Sen-Biao Fang; Qin-Ying Li; Yan-Chao Wu
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Design, synthesis and structure-activity relationships of novel 15-membered macrolides: Quinolone/quinoline-containing sidechains tethered to the C-6 position of azithromycin acylides Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-14 Bing-Zhi Fan; Hiroshi Hiasa; Wei Lv; Scott Brody; Zhao-Yong Yang; Courtney Aldrich; Mark Cushman; Jian-Hua Liang
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Antitumor activity and structure-activity relationship of heparanase inhibitors: Recent advances Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-14 Kaishuo Fu; Zhifeng Bai; LanLan Chen; Wenchong Ye; Meizhu Wang; Jilian Hu; Chunhui Liu; Zhou Wen
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In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-14 Dongwei Kang; Da Feng; Lanlan Jing; Yanying Sun; Fenju Wei; Xiangyi Jiang; Gaochan Wu; Erik De Clercq; Christophe Pannecouque; Peng Zhan; Xinyong Liu
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Synthesis and biological evaluation of gold(III) Schiff base complexes for the treatment of hepatocellular carcinoma through attenuating TrxR activity Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-14 Mianli Bian; Xin Wang; Ying Sun; Wukun Liu
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Discovery of small molecules targeting GRP78 for antiangiogenic and anticancer therapy Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-13 Yixue Qiao; Charlotte Dsouza; Abigail Ann Matthews; Yan Jin; Wan He; Jian Bao; Faqin Jiang; Ritu Chandna; Ruowen Ge; Lei Fu
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Development of potent inhibitors of the human microsomal epoxide hydrolase Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-13 Bogdan Barnych; Nalin Singh; Sophie Negrel; Yue Zhang; Damien Magis; Capucine Roux; Xiude Hua; Zhewen Ding; Christophe Morisseau; Dean J. Tantillo; Justin B. Siegel; Bruce D. Hammock
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A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-13 Andreas Sellmer; Bernadette Pilsl; Mandy Beyer; Herwig Pongratz; Lukas Wirth; Sigurd Elz; Stefan Dove; Sven Julian Henninger; Karsten Spiekermann; Harald Polzer; Susan Klaeger; Bernhard Kuster; Frank D. Böhmer; Heinz-Herbert Fiebig; Oliver H. Krämer; Siavosh Mahboobi
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N-benzyl 4,4-disubstituted piperidines as a potent class of influenza H1N1 virus inhibitors showing a novel mechanism of hemagglutinin fusion peptide interaction Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-13 Sonia de Castro; Tiziana Ginex; Evelien Vanderlinden; Manon Laporte; Annelies Stevaert; José Cumella; Federico Gago; María José Camarasa; F. Javier Luque; Lieve Naesens; Sonsoles Velazquez
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Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-12 Jin Zhang; Ling Zou; Tang pan; Dabo Pan; Zhendan He; Dahong Yao
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Structure-activity relationships of triazole-benzodioxine inhibitors of cathepsin X Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-12 Urša Pečar Fonović; Damijan Knez; Martina Hrast; Nace Zidar; Matic Proj; Stanislav Gobec; Janko Kos
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Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-10 Chen Zhu; Xinwei Li; Bangyi Zhao; Weiqing Peng; Wei Li; Wei Fu
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Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-10 Vikas Sharma; Rajiv Kumar; Andrea Angeli; Claudiu T. Supuran; Pawan K. Sharma
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Design, synthesis and bioactivity study of N-salicyloyl tryptamine derivatives as multifunctional agents for the treatment of neuroinflammation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-09 Xiaohong Fan; Junfang Li; Xuemei Deng; Yingmei Lu; Yiyue Feng; Shumeng Ma; Huaixiu Wen; Quanyi Zhao; Wen Tan; Tao Shi; Zhen Wang
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Chalcone hybrids as privileged scaffolds in antimalarial drug discovery: A key review Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-09 Hua-Li Qin; Zai-Wei Zhang; Ravindar Lekkala; Hamed Alsulami; K.P. Rakesh
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Development of a novel nitric oxide (NO) production inhibitor with potential therapeutic effect on chronic inflammation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-08 Youzhe Yang; Zhe Wei; Alexander Tobias Teichmann; Frank Heinrich Wieland; Amu Wang; Xiangui Lei; Yue Zhu; Jinxiang Yin; Tiantian Fan; Li Zhou; Chao Wang; Lijuan Chen
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Anti-norovirus activity of C7-modified 4-amino-pyrrolo[2,1-f][1,2,4]triazine C-nucleosides Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-07 Qingfeng Li; Elisabetta Groaz; Joana Rocha-Pereira; Johan Neyts; Piet Herdewijn
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Discovery of orally active indirubin-3′-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-06 Pyeonghwa Jeong; Yeongyu Moon; Je-Heon Lee; So-Deok Lee; Jiyeon Park; Jungeun Lee; Jiheon Kim; Hyo Jeong Lee; Na Yoon Kim; Jungil Choi; Jeong Doo Heo; Ji Eun Shin; Hyun Woo Park; Yoon-Gyoon Kim; Sun-Young Han; Yong-Chul Kim
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A glutathione-responsive photosensitizer with fluorescence resonance energy transfer characteristics for imaging-guided targeting photodynamic therapy Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-06 Jing-Jing Cao; Ming-Shan Zhang; Xiao-Qiang Li; De-Chao Yang; Gan Xu; Jian-Yong Liu
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Non-polyphenolic natural inhibitors of amyloid aggregation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-05 Liang Ma; Chen Yang; Jiaojiao Zheng; Yuchen Chen; Yushuo Xiao; Kun Huang
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Research progress on sirtuins family members and cell senescence Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-05 Ting Wang; Yujue Wang; Li Liu; Zhongliang Jiang; Xingxing Li; Rongsheng Tong; Jun He; Jianyou Shi
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Discovery of pyridine tetrahydroisoquinoline thiohydantoin derivatives with low blood-brain barrier penetration as the androgen receptor antagonists Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-05 Xi Xu; Qianming Du; Ying Meng; Zhiyu Li; Hongxi Wu; Yan Li; Zhili Zhao; Raoling Ge; Xiaoyu Lu; Siqi Xue; Xijing Chen; Yong Yang; Jubo Wang; Jinlei Bian
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Design and synthesis of selective degraders of EGFRL858R/T790M mutant Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-05 Xin Zhang; Fang Xu; Linjiang Tong; Tao Zhang; Hua Xie; Xiaoyun Lu; Xiaomei Ren; Ke Ding
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Design, preparation and evaluation of different branched biotin modified liposomes for targeting breast cancer Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-05 Baolan Tang; Yao Peng; Qiming Yue; Yanchi Pu; Ru Li; Yi Zhao; Li Hai; Li Guo; Yong Wu
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True or false? Challenges and recent highlights in the development of aspirin prodrugs Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-03 Steffan Willetts; David W. Foley
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Synthesis of antiplatelet ortho-carbonyl hydroquinones with differential action on platelet aggregation stimulated by collagen or TRAP-6 Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-02 Diego Méndez; Félix A. Urra; Juan Pablo Millas-Vargas; Marcelo Alarcón; Julio Rodriguez-Lavado; Iván Palomo; Andrés Trostchansky; Ramiro Araya-Maturana; Eduardo Fuentes
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Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-03-02 Ling-Ling Yang; Hua-Li Wang; Yu-Hang Yan; Sha Liu; Zhu-Jun Yu; Meng-Yi Huang; Yubin Luo; Xi Zheng; Yamei Yu; Guo-Bo Li
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Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-02-29 Hui-Ju Tseng; Mei-Hsiang Lin; Young-Ji Shiao; Ying-Chen Yang; Jung-Chun Chu; Chun-Yung Chen; Yi-Ying Chen; Tony Eight Lin; Chih-Jou Su; Shiow-Lin Pan; Liang-Chieh Chen; Chen-Yu Wang; Kai-Cheng Hsu; Wei-Jan Huang
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Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-02-29 Ning Sun; Chaowei Ren; Ying Kong; Hui Zhong; Jinju Chen; Yan Li; Jianshui Zhang; Yuedong Zhou; Xing Qiu; Haifan Lin; Xiaoling Song; Xiaobao Yang; Biao Jiang
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Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-02-28 Alexandra Knox; Christina Kalchschmid; Daniela Schuster; Francesca Gaggia; Claudia Manzl; Daniel Baecker; Ronald Gust
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Cyclometalated Ir(III)-8-oxychinolin complexes acting as red-colored probes for specific mitochondrial imaging and anticancer drugs Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-02-28 Ting Meng; Qi-Pin Qin; Zi-Lu Chen; Hua-Hong Zou; Kai Wang; Fu-Pei Liang
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Structure-thermodynamics-relationships of hepatitis C viral NS3 protease inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-02-28 Rachel M. Wypych; Steven R. LaPlante; Peter W. White; Stephen F. Martin
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