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Xanthenes in Medicinal Chemistry – Synthetic strategies and biological activities Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-04 Miguel Maia; Diana I.S.P. Resende; Fernando Durães; Madalena M.M. Pinto; Emília Sousa
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Recent accomplishments on the synthetic/biological facets of pharmacologically active 1H-1,2,3-triazoles Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-03 Sumit Kumar; Bharvi Sharma; Vishu Mehra; Vipan Kumar
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Synergistic effects of Curcumin and its Analogs with other Bioactive Compounds: A Comprehensive Review Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-03 Maryam Sadat Hosseini-Zare; Mozhgan Sarhadi; Mehdi Zarei; Ramasamy Thilagavathi; Chelliah Selvam
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Discovery of Novel PARP/PI3K Dual Inhibitors with High Efficiency against BRCA-proficient Triple Negative Breast Cancer Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-03 Junwei Wang; Guangchao He; Hui Li; Yiran Ge; Shuping Wang; Yungen Xu; Qihua Zhu
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Development of 2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of Aldehyde Dehydrogenase 1A (ALDH1A) as potential adjuncts to ovarian cancer chemotherapy Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-03 Brandt C. Huddle; Edward Grimley; Mikhail Chtcherbinine; Cameron D. Buchman; Cyrus Takahashi; Bikash Debnath; Stacy C. McGonigal; Shuai Mao; Siwei Li; Jeremy Felton; Shu Pan; Bo Wen; Duxin Sun; Nouri Neamati; Ronald J. Buckanovich; Thomas D. Hurley; Scott D. Larsen
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Design, synthesis, and biodistribution studies of new analogues of marine alkaloids: Potent in vitro and in vivo fungicidal agents against Candida spp. Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-03 Jéssica Tauany Andrade; William Gustavo Lima; Jaqueline França Sousa; Aline Aparecida Saldanha; Nívea Pereira De Sá; Fernanda Barbara Morais; Mayra Karla Prates Silva; Gustavo Henrique Ribeiro Viana; Susana Johann; Adriana Cristina Soares; Leonardo Allan Araújo; Simone Odília Antunes Fernandes; Valbert Nascimento Cardoso; Jaqueline Maria Siqueira Ferreira
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Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT6 receptor antagonist with therapeutic interest in Alzheimer's disease Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-03 François-Xavier Toublet; Julien Lalut; Bérénice Hatat; Cédric Lecoutey; Audrey Davis; Marc Since; Sophie Corvaisier; Thomas Freret; Jana Sopková-de Oliveira Santos; Sylvie Claeysen; Michel Boulouard; Patrick Dallemagne; Christophe Rochais
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Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-03 Katja Silbermann; Jiyang Li; Vigneshwaran Namasivayam; Sven Marcel Stefan; Michael Wiese
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Conjugation of Tacrine with Genipin Derivative not only Enhances Effects on AChE but also Leads to Autophagy against Alzheimer’s Disease Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-02 Rongtian Lin; Shuwen Rao; Yanbing Li; Lei Zhang; Liyu Xu; Yepu He; Zhijun Liu; Heru Chen
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Diverse Chemical Space of Indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-02 Rahul Singh; Deepak B. Salunke
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Structures/Cytotoxicity/Selectivity Relationship of Natural Steroidal Saponins against GSCs and Primary Mechanism of Tribulosaponin A Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-02 Zhi Dai; Hui Liu; Bei Wang; Dong Yang; Yan-Yan Zhu; Huan Yan; Pei-Feng Zhu; Ya-Ping Liu; Hui-Cheng Chen; Yun-li Zhao; Li-Xing Zhao; Xu-Dong Zhao; Hai-Yang Liu; Xiao-Dong Luo
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Research progress in biological activities of isochroman derivatives Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-02 Zefeng Zhao; Kaiwen Kang; Jiangxin Yue; Xiaotong Ji; Haifa Qiao; Peinan Fan; Xiaohui Zheng
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Undecaprenol Kinase: Function, Mechanism and Substrate Specificity of a Potential Antibiotic Target Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-02 Brad R. Baker; Callum M. Ives; Ashley Bray; Martin Caffrey; Stephen A. Cochrane
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4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle: a promising scaffold towards bioactive molecules Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-02 Fabiana Plescia; Benedetta Maggio; Giuseppe Daidone; Demetrio Raffa
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Discovery of indazole-pyridinone derivatives as a novel class of potent and selective MNK1/2 kinase inhibitors that protecting against endotoxin-induced septic shock Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-01 Agnieszka Dreas; Katarzyna Kucwaj-Brysz; Karolina Pyziak; Urszula Kulesza; Ewelina Wincza; Charles-Henry Fabritius; Kinga Michalik; Ewelina Gabor-Worwa; Aniela Gołas; Mariusz Milik; Magdalena Masiejczyk; Eliza Majewska; Kazimiera Pysniak; Urszula Wojcik-Trechcinska; Zuzanna Sandowska-Markiewicz; Krzysztof Brzózka; Jerzy Ostrowski; Tomasz Rzymski; Michal Mikula
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Non-hydroxamate inhibitors of 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR): a critical review and future perspective Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-01 Sharyu Kesharwani; Sandeep Sundriyal
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Potentials of nanotechnology in treatment of methicillin-resistant Staphylococcus aureus Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-01 Yujie Gao; Yuan Chen; Yubin Cao; Anchun Mo; Qiang Peng
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Ruthenium compounds as potential therapeutic agents for Type 2 Diabetes Mellitus Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-12-01 Sanam Maikoo; Daniel Makayane; Irvin Noel Booysen; Phikelelani Ngubane; Andile Khathi
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Discovery of 7-aminophenanthridin-6-one as a new scaffold for matrix metalloproteinase inhibitors with multitarget neuroprotective activity Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-30 Damiano Rocchi; Cristina Blázquez-Barbadillo; Mariangela Agamennone; Antonio Laghezza; Paolo Tortorella; David Vicente-Zurdo; Noelia Rosales-Conrado; Paula Moyano; Javier del Pino; Juan F. González; J. Carlos Menéndez
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Discovery of Novel CA-4 Analogs as Dual Inhibitors of Tubulin Polymerization and PD-1/PD-L1 Interaction for Cancer Treatment Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-30 Xuchao Yang; Binbin Cheng; Yao Xiao; Mingming Xue; Ting Liu; Hao Cao; Jianjun Chen
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Design and structural optimization of novel 2H-benzo[h]chromene derivatives that target AcrB and reverse bacterial multidrug resistance Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-27 Yinhu Wang; Rawaf Alenazy; Xinjie Gu; Steven W. Polyak; Panpan Zhang; Matthew J. Sykes; Na Zhang; Henrietta Venter; Shutao Ma
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Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp3 values and favorable drug-like properties Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-27 Xiangyi Jiang; Boshi Huang; Fisayo A. Olotu; Jing Li; Dongwei Kang; Zhao Wang; Erik De Clercq; Mahmoud E.S. Soliman; Christophe Pannecouque; Xinyong Liu; Peng Zhan
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Synthesis and in vitro evaluation of novel spiroketopyrazoles as acetyl-CoA carboxylase inhibitors and potential antitumor agents Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-27 Tonghui Huang; Xin Wu; Shirong Yan; Tianya Liu; Xiaoxing Yin
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Discovery of Novel Cell-penetrating and Tumor-targeting Peptide-Drug Conjugate (PDC) for Programmable Delivery of Paclitaxel and Cancer Treatment Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-27 Xin Deng; Ruiyao Mai; Chenyu Zhang; Dianbao Yu; Yichang Ren; Gang Li; Binbin Cheng; Ling Li; Zhiqiang Yu; Jianjun Chen
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A Greener Protocol for the Synthesis of Phosphorochalcogenoates: Antioxidant and Free Radical Scavenging Activities Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-27 Daniela H. Mailahn; Lucas E.B. Iarocz; Patrick C. Nobre; Gelson Perin; Airton Sinott; Ana Paula Pesarico; Paloma T. Birmann; Lucielli Savegnago; Márcio S. Silva
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18F-Labeled Radiotracers for In Vivo Imaging of DREADD with Positron Emission Tomography Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-25 Feng Hu; Patrick J. Morris; Jordi Bonaventura; Hong Fan; William B. Mathews; Daniel P. Holt; Sherry Lam; Matthew Boehm; Robert F. Dannals; Martin G. Pomper; Mike Michaelides; Andrew G. Horti
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A Review: Biologically active 3,4-heterocycle-fused coumarins Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-25 Fatemeh Salehian; Hamid Nadri; Leili Jalili-Baleh; Leila Youseftabar-Miri; Syed Nasir Abbas Bukhari; Alireza Foroumadi; Tuba Tüylü Küçükkilinç; Mohammad Sharifzadeh; Mehdi Khoobi
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Radiotracers for positron emission tomography (PET) targeting tumour-associated carbonic anhydrase isoforms Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-25 Valeria Burianova; Stanislav Kalinin; Claudiu T. Supuran; Mikhail Krasavin
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Imidazo[1,2-a]quinoxalines for melanoma treatment with original mechanism of action Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-24 Cindy Patinote; Carine Deleuze-Masquéfa; Kamel Hadj Kaddour; Laure-Anaïs Vincent; Romain Larive; Zahraa Zghaib; Jean-François Guichou; Mona Diab Assaf; Pierre Cuq; Pierre-Antoine Bonnet
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Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-24 Katarzyna Szczepańska; Steffen Pockes; Sabina Podlewska; Carina Höring; Kamil Mika; Gniewomir Latacz; Marek Bednarski; Agata Siwek; Tadeusz Karcz; Martin Nagl; Merlin Bresinsky; Denise Mönnich; Ulla Seibel; Kamil J. Kuder; Magdalena Kotańska; Holger Stark; Sigurd Elz; Katarzyna Kieć-Kononowicz
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Design, synthesis and biological evaluation of novel scaffold benzo[4,5]imidazo [1,2-a]pyrazin-1-amine: towards adenosine A2A receptor (A2A AR) antagonist Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-24 G. Lakshma Reddy; Rupam Sarma; Shuhao Liu; Weifeng Huang; Jinping Lei; Jiasheng Fu; Wenhao Hu
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Angel or Devil ? - CDK8 as the new drug target Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-24 Dan Wu; Zhaoyan Zhang; Xing Chen; Yaoyao Yan; Xinhua Liu
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Outline of gelatinase inhibitors as anti-cancer agents: A patent mini-review for 2010-present Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-24 Sandip Kumar Baidya; Sk. Abdul Amin; Tarun Jha
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Development of Mcl-1 Inhibitors for Cancer Therapy Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-24 Arvind Negi; Paul V. Murphy
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Engagement of Phytoestrogens in Breast Cancer suppression: Structural classification and mechanistic approach Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-24 Ankur Kumar Tanwar; Neha Dhiman; Amit Kumar; Vikas Jaitak
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New derivatives of 4'-phenyl-2,2':6',2''-terpyridine as promising anticancer agents Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-23 Katarzyna Malarz; Dawid Zych; Robert Gawecki; Michał Kuczak; Robert Musioł; Anna Mrozek-Wilczkiewicz
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Paracetamol analogues conjugated by FAAH induce TRPV1-mediated antinociception without causing acute liver toxicity Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-21 Johan L. Å.Nilsson; Christophe Mallet; Kiseko Shionoya; Anders Blomgren; Anders P. Sundin; Lars Grundemar; Ludivine Boudieu; Anders Blomqvist; Alain Eschalier; Ulf J. Nilsson; Peter M. Zygmunt
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Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-21 Yuanyuan Wang; Hao Ma; Jiaxuan Huang; Zhengguang Yao; Jianqiang Yu; Wannian Zhang; Lichao Zhang; Zhibin Wang; Chunlin Zhuang
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Targeting the Kv11.1 (hERG) channel with allosteric modulators. Synthesis and biological evaluation of three novel series of LUF7346 derivatives Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-21 Jacobus P.D. van Veldhoven; Giulia Campostrini; Constantijn J.E. van Gessel; Dorien Ward-van Oostwaard; Rongfang Liu; Christine L. Mummery; Milena Bellin; Adriaan P. IJzerman
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Handling Drug-Target Selectivity: A Study on Ureido Containing Carbonic Anhydrase Inhibitors Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-21 Ozlem Akgul; Srishti Singh; Jacob T. Andring; Robert McKenna; Silvia Selleri; Fabrizio Carta; Andrea Angeli; Claudiu T. Supuran
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Synthesis and Anticancer Activity Evaluation of Naphthalene-Substituted Triazole Spirodienones Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-21 Lan Luo; Jing Jing Jia; Qiu Zhong; Xue Zhong; Shilong Zheng; Guangdi Wang; Ling He
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Discovery of Tetrahydroquinolines and Benzomorpholines as Novel Potent RORγt Agonists Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-19 Yuehan Xia; Mingcheng Yu; Yunpeng Zhao; Li Xia; Yafei Huang; Nannan Sun; Meiqi Song; Huimin Guo; Yunyi Zhang; Di Zhu; Qiong Xie; Yonghui Wang
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Melatonin Derivatives Combat with Inflammation-related Cancer by Targeting the Main Culprit STAT3 Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-17 Shumeng Ma; Longqing Zhu; Xiaohong Fan; Tian Luo; Dan Liu; Ziyi Liang; Xiaoling Hu; Tao Shi; Wen Tan; Zhen Wang
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Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-17 Yufei Han; Desheng Huang; Sicong Xu; Lingling Li; Ye Tian; Shuo Li; Cong Chen; Yingxiu Li; Yanping Sun; Yunlei Hou; Yongjun Sun; Mingze Qin; Ping Gong; Zibin Gao; Yanfang Zhao
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Targeting KRAS Mutant Cancers by Preventing Signaling Transduction in the MAPK Pathway Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-17 Claudia Korzeniecki; Ronny Priefer
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Synthesis and Structure-Activity Studies of Novel Anhydrohexitol-based Leucyl-tRNA Synthetase Inhibitors Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-16 Dries De Ruysscher; Luping Pang; Stijn M.G. Lenders; Davie Cappoen; Paul Cos; Jef Rozenski; Sergei V. Strelkov; Stephen D. Weeks; Arthur Van Aerschot
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The New Opportunities in Medicinal Chemistry of Fourth-Generation EGFR Inhibitors to Overcome C797S Mutation Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-16 Jie He; Zhihui Zhou; Xin Sun; Zunhua Yang; Pengwu Zheng; Shan Xu; Wufu Zhu
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Pyrido[2, 3-d]pyrimidin-7(8H)-ones as New Selective Orally Bioavailable Threonine Tyrosine Kinase (TTK) Inhibitors Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-16 Minhao Huang; Yongjun Huang; Jing Guo; Lei Yu; Yu Chang; Xiaolu Wang; Jinfeng Luo; Yanhui Huang; Zhengchao Tu; Xiaoyun Lu; Yong Xu; Zhimin Zhang; Zhang Zhang; Ke Ding
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Optimization of novel oxidative DIMs as Nur77 modulators of the Nur77-Bcl-2 Apoptotic Pathway Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-13 Xuhuang Tu; Xiaohui Chen; Dongliang Zhang; Meichun Gao; Jingmei Liang; Guoliang Bao; Jie Zhang; Shuangzhou Peng; Xiaokun Zhang; Zhiping Zeng; Ying Su
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Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFRL858R/T790M inhibitors Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-13 Jianheng Li; Baijiao An; Xianheng Song; Qianzhong Zhang; Chun Chen; Shuxian Wei; Runzhu Fan; Xingshu Li; Yong Zou
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Dual Nicotinamide Phosphoribosyltransferase and Epidermal Growth Factor Receptor Inhibitors for the Treatment of Cancer Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-13 Wanheng Zhang; Kuojun Zhang; Yiwu Yao; Yunyao Liu; Yong Ni; Chenzhong Liao; Zhengchao Tu; Yatao Qiu; Dexiang Wang; Dong Chen; Lei Qiang; Zheng Li; Sheng Jiang
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Evolution in non-peptide α-helix mimetics on the road to effective protein-protein interaction modulators Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-12 Sergio Algar; Mercedes Martín-Martínez; Rosario González-Muñiz
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Development of programmable gemcitabine-GnRH pro-drugs bearing linker controllable “click” oxime bond tethers and preclinical evaluation against prostate cancer Eur. J. Med. Chem. (IF 5.572) Pub Date : 2020-11-12 Eirinaios I. Vrettos; Theodoros Karampelas; Nisar Sayyad; Anastasia Kougioumtzi; Nelofer Syed; Timothy Crook; Carol Murphy; Constantin Tamvakopoulos; Andreas G. Tzakos
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