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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-24 Agnieszka Siebert; Grzegorz Cholewiński; Piotr Trzonkowski; Janusz Rachon
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Design, synthesis and structure-activity relationships of 4-phenyl-1H-1,2,3-Triazole phenylalanine derivatives as novel HIV-1 capsid inhibitors with promising antiviral activities Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-24 Lin Sun; Tianguang Huang; Alexej Dick; Megan E. Meuser; Waleed A. Zalloum; Chin Ho Chen; Xiao Ding; Ping Gao; Simon Cocklin; Kuo-Hsiung Lee; Peng Zhan; Xinyong Liu
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Structural features and functional activities of benzimidazoles as NOD2 antagonists Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-24 Samo Guzelj; Martina Gobec; Dunja Urbančič; Irena Mlinarič-Raščan; Emanuela Corsini; Žiga Jakopin
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Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-23 Ritu Ojha; Kunal Nepali; Chun-Han Chen; Kuo-Hsiang Chuang; Tung-Yun Wu; Tony Eight Lin; Kai-Cheng Hsu; Min-Wu Chao; Mei-Jung Lai; Mei-Hsiang Lin; Han-Li Huang; Chao-Di Chang; Shiow-Lin Pan; Mei-Chuan Chen; Jing-Ping Liou
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Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-23 Meng Yu; Minghui Zeng; Zhaoping Pan; Fengbo Wu; Li Guo; Gu He
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Discovery, synthesis, and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-22 Chengbo Xu; Yijing Xin; Minghua Chen; Mingyu Ba; Qinglan Guo; Chenggen Zhu; Ying Guo; Jiangong Shi
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Identification of descriptors for structure-activity relationship in ruthenium (II) mixed compounds with antiparasitic activity Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-22 Erika Lorena Cedillo-Gutiérrez; Luis Felipe Hernández-Ayala; Carolina Torres-Gutiérrez; Miguel Reina; Marcos Flores-Alamo; Julio C. Carrero; Víctor M. Ugalde-Saldívar; Lena Ruiz-Azuara
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Bis(vinylsulfonyl)piperazines as efficient linkers for highly homogeneous antibody-drug conjugates Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-22 Rong Huang; Yao Sheng; Ding Wei; Jianghui Yu; Hongli Chen; Biao Jiang
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Optimization of EphA2 antagonists based on a lithocholic acid core led to the identification of UniPR505, a new 3α-carbamoyloxy derivative with antiangiogenetic properties Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-22 Matteo Incerti; Simonetta Russo; Miriam Corrado; Carmine Giorgio; Vigilio Ballabeni; Paola Chiodelli; Marco Rusnati; Laura Scalvini; Donatella Callegari; Riccardo Castelli; Federica Vacondio; Francesca Ferlenghi; Massimiliano Tognolini; Alessio Lodola
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Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-22 Raphaël Bolteau; Florian Descamps; Mohamed Ettaoussi; Daniel H. Caignard; Philippe Delagrange; Patricia Melnyk; Saïd Yous
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Design, synthesis and biological evaluation of 1-alkyl-5/6-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-1H-indole-3-carbonitriles as novel xanthine oxidase inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-21 Jun Gao; Xuegui Liu; Bing Zhang; Qing Mao; Zhuo Zhang; Qian Zou; Xiwen Dai; Shaojie Wang
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Novel nitric oxide-releasing derivatives of triptolide as antitumor and anti-inflammatory agents: Design, synthesis, biological evaluation, and nitric oxide release studies Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-21 Zang Yingda; Fangfang Lai; Junmin Fu; Chuangjun Li; Jie Ma; Chengjuan Chen; Ke Liu; Tiantai Zhang; Xiaoguang Chen; Dongming Zhang
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Simple amphiphilic α-hydrazido acids: Rational design, synthesis, and in vitro bioactivity profile of a novel class of potential antimicrobial compounds Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-21 Paolo Amabili; Francesca Biavasco; Andrea Brenciani; Barbara Citterio; Dario Corbisiero; Lucia Ferrazzano; Simona Fioriti; Giulia Guerra; Mario Orena; Samuele Rinaldi
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Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-21 Chunhui Cheng; Fan Yun; Sadeeq Ullah; Qipeng Yuan
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New azole antifungals with a fused triazinone scaffold Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-20 David Montoir; Rémi Guillon; Sophie Gazzola; Isabelle Ourliac-Garnier; Kossi Efouako Soklou; Alain Tonnerre; Carine Picot; Aurélien Planchat; Fabrice Pagniez; Patrice Le Pape; Cédric Logé
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Celastrol: Progresses in structure-modifications, structure-activity relationships, pharmacology and toxicology Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-20 Wei Hou; Bo Liu; Hongtao Xu
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Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-19 Wenting Zhao; Bin Wang; Yuke Liu; Lei Fu; Li Sheng; Hongyi Zhao; Yu Lu; Dongfeng Zhang
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Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-18 Huoming Huang; Wenli Wang; Xuejun Xu; Chen Zhu; Yujun Wang; Jinggen Liu; Wei Li; Wei Fu
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1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226 Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-17 Heba F. Ashour; Laila A. Abou-zeid; Magda A. -A. El-Sayed; Khalid B. Selim
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Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-16 Ehab M. Gedawy; Asmaa E. Kassab; Ahmed M. El Kerdawy
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Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC) Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-14 Hao Zhang; Hong-Yi Zhao; Xiao-Xiao Xi; Yan-Jie Liu; Minhang Xin; Shuai Mao; Jun-Jie Zhang; A-Xin Lu; San-Qi Zhang
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Synthesis, mechanisms of action, and toxicity of novel aminophosphonates derivatives conjugated irinotecan in vitro and in vivo as potent antitumor agents Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-14 Xiaochao Huang; Meng Wang; Qinghong You; Jing Kong; Haijiang Zhang; Chunhao Yu; Yanming Wang; Hengshan Wang; Rizhen Huang
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Synthesis, biological evaluation and in silico modeling of novel integrase strand transfer inhibitors (INSTIs) Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-13 Andrey A. Ivashchenko; Yan A. Ivanenkov; Angela G. Koryakova; Ruben N. Karapetian; Oleg D. Mitkin; Vladimir A. Aladinskiy; Dmitry V. Kravchenko; Nikolai P. Savchuk; Alexander V. Ivashchenko
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Design, synthesis and biological evaluation of new ganglioside GM3 analogues as potential agents for cancer therapy Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-13 Changping Zheng; Ruyi Huang; Teodora Bavaro; Marco Terreni; Matthieu Sollogoub; Jianhua Xu; Yongmin Zhang
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Synthetic tumor-specific antigenic peptides with a strong affinity to HLA-A2 elicit anti-breast cancer immune response through activating CD8+ T cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-11 Wei Shi; Qianqian Qiu; Zhenzhen Tong; Weiwei Guo; Feng Zou; Ziying Feng; Yao Wang; Wenlong Huang; Hai Qian
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Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-11 Xiaohan Song; Pu Sun; Jiang Wang; Wei Guo; Yi Wang; Ling-hua Meng; Hong Liu
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Natural heat shock protein 90 inhibitors in cancer and inflammation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-11 Thadeu E.M.M. Costa; Nulgumnalli M. Raghavendra; Carmen Penido
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Synthesis and SARs of dopamine derivatives as potential inhibitors of influenza virus PAN endonuclease Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-11 Yixian Liao; Yilu Ye; Sumei Li; Yilian Zhuang; Liye Chen; Jianxin Chen; Zining Cui; Lijian Huo; Shuwen Liu; Gaopeng Song
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Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-10 Nazar Trotsko; Joanna Golus; Paulina Kazimierczak; Agata Paneth; Agata Przekora; Grazyna Ginalska; Monika Wujec
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Identification of a 2,4-diaminopyrimidine scaffold targeting Trypanosoma brucei pteridine reductase 1 from the LIBRA compound library screening campaign Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-10 Pasquale Linciano; Gregorio Cullia; Chiara Borsari; Matteo Santucci; Stefania Ferrari; Gesa Witt; Sheraz Gul; Maria Kuzikov; Bernhard Ellinger; Nuno Santarém; Anabela Cordeiro da Silva; Paola Conti; Maria Laura Bolognesi; Marinella Roberti; Federica Prati; Francesca Bartoccini; Michele Retini; Giovanni Piersanti; Maria Paola Costi
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Oxadiazolylthiazoles as novel and selective antifungal agents Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-10 Mohamed Hagras; Ehab A. Salama; Ahmed M. Sayed; Nader S. Abutaleb; Ahmed Kotb; Mohamed N. Seleem; Abdelrahman S. Mayhoub
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β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-10 Azizah M. Malebari; Darren Fayne; Seema M. Nathwani; Fiona O'Connell; Sara Noorani; Brendan Twamley; Niamh M. O'Boyle; Jacintha O'Sullivan; Daniela M. Zisterer; Mary J. Meegan
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The development of a novel transforming growth factor-β (TGF-β) inhibitor that disrupts ligand-receptor interactions Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-09 Han Wu; Yu Sun; Wee Lin Wong; Jiajia Cui; Jingyang Li; Xuefu You; Lee Fah Yap; Yu Huang; Wei Hong; Xinyi Yang; Ian Paterson; Hao Wang
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Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-09 Madeleine Gold; Leonhard Köhler; Clarissa Lanzloth; Ion Andronache; Shrikant Anant; Prasad Dandawate; Bernhard Biersack; Rainer Schobert
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Dual-functional conjugates improving cancer immunochemotherapy by inhibiting tubulin polymerization and indoleamine-2,3-dioxygenase Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-09 Shixian Hua; Feihong Chen; Xinyi Wang; Shaohua Gou
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Anticancer activity of 4′-phenyl-2,2':6′,2″-terpyridines – Behind the metal complexation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-09 Katarzyna Malarz; Dawid Zych; Michał Kuczak; Robert Musioł; Anna Mrozek-Wilczkiewicz
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Synthesis and pharmacological evaluation of chlorin derivatives for photodynamic therapy of cholangiocarcinoma Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-09 Ying-Hua Gao; Man-Yi Li; Faiza Sajjad; Jin-Hai Wang; Faiza Meharban; Malaz Abdelazeem Gadoora; Yi-Jia Yan; Tebello Nyokong; Zhi-Long Chen
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Total synthesis, chemical modification and structure-activity relationship of bufadienolides Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-08 Yue- Zhong; Chao- Zhao; Wen-Yu Wu; Tian-Yuan Fan; Nian-Guang Li; Min- Chen; Jin-Ao Duan; Zhi-Hao Shi
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Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-08 Jaime Franco; Laura Scarone; Marcelo A. Comini
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Artemisinin-derived hybrids and their anticancer activity Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-08 Feng Gao; Zhou Sun; Fangong Kong; Jiaqi Xiao
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Discovery of novel pyrido-pyrrolidine hybrid compounds as alpha-glucosidase inhibitors and alternative agent for control of type 1 diabetes Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-07 Tania Luthra; Venkanna Banothu; Uma Adepally; Krishna Kumar; Swathi M; Saikat Chakrabarti; Srinivas R. Maddi; Subhabrata Sen
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Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-07 Hilal Doğan; Şengül Dilem Doğan; Miyase Gözde Gündüz; Vagolu Siva Krishna; Christian Lherbet; Dharmarajan Sriram; Onur Şahin; Emin Sarıpınar
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Therapeutic potentials of curcumin in the treatment of glioblstoma Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-07 Zahra Shabaninejad; Mohammad Hossein Pourhanifeh; Ahmad Movahedpour; Reza Reza Mottaghi; Ali Nickdasti; Erfan Mortezapour; Alimohammad Shafiee; Sarah Hajighadimi; Sanaz Moradizarmehri; Mohammad Sadeghian; Seyed Mojtaba Mousavi; Hamed Mirzaei
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Design and synthesis of fluorescent ligands for the detection of cannabinoid type 2 receptor (CB2R) Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-07 Francesco Spinelli; Roberta Giampietro; Angela Stefanachi; Chiara Riganti; Joanna Kopecka; Francesca Serena Abatematteo; Francesco Leonetti; Nicola Antonio Colabufo; Giuseppe Felice Mangiatordi; Orazio Nicolotti; Maria Grazia Perrone; José Brea; María Isabel Loza; Vittoria Infantino; Carmen Abate; Marialessandra Contino
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Novel modified leucine and phenylalanine dipeptides modulate viability and attachment of cancer cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-07 Radek Jorda; Pratibha Magar; Denisa Hendrychová; Karel Pauk; Michal Dibuš; Eliška Pilařová; Aleš Imramovský; Vladimír Kryštof
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Preparation and evaluation of 99mTc-Labeled HYNIC-Palbociclib analogs for cyclin-dependent kinase 4/6-positive tumor imaging Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-03 Qianqian Gan; Xiaoqing Song; Xuran Zhang; Junbo Zhang
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Synthesis and biological assessment of a Ruthenium(II) cyclopentadienyl complex in breast cancer cells and on the development of zebrafish embryos Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-03 Golara Golbaghi; Irène Pitard; Matthieu Lucas; Mohammad Mehdi Haghdoost; Yossef López de los Santos; Nicolas Doucet; Shunmoogum A. Patten; J. Thomas Sanderson; Annie Castonguay
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C6–O-alkylated 7-deaza inosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-03 Fabian Hulpia; Jakob Bouton; Gustavo D. Campagnaro; Ibrahim A. Alfayez; Dorien Mabille; Louis Maes; Harry P. de Koning; Guy Caljon; Serge Van Calenbergh
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Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-02 Garrett S. Gibbons; Amarraj Chakraborty; Sierrah M. Grigsby; Afoma C. Umeano; Chenzhong Liao; Omar Moukha-Chafiq; Vibha Pathak; Bini Mathew; Young‐Tae Lee; Yali Dou; Stephan C. Schürer; Robert C. Reynolds; Timothy S. Snowden; Zaneta Nikolovska-Coleska
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Dual-target kinase drug design: Current strategies and future directions in cancer therapy Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-02 Dejuan Sun; Yuqian Zhao; Shouyue Zhang; Lan Zhang; Bo Liu; Liang Ouyang
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Molecular design, synthesis, and biological evaluation of bisamide derivatives as cyclophilin A inhibitors for HCV treatment Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-02 Jinhe Han; Hye Won Lee; Yifeng Jin; Daulat B. Khadka; Suhui Yang; Xiaoli Li; Meehyein Kim; Won-Jea Cho
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Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-02 Li Zhou; Wenming Chen; Chenyang Cao; Yonghui Shi; Wenchong Ye; Jiliang Hu; LingLi Wang; Wen Zhou
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Design, synthesis and biological evaluation of naphthalenebenzimidizole platinum (II) complexes as potential antitumor agents Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-02 Gui-Bin Liang; Yan-Cheng Yu; Jian-Hua Wei; Wen-Bin Kuang; Zhen-Feng Chen; Ye Zhang
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Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-02 Mohamed A. Said; Wagdy M. Eldehna; Alessio Nocentini; Samar H. Fahim; Alessandro Bonardi; Abdullah A. Elgazar; Vladimír Kryštof; Dalia H. Soliman; Hatem A. Abdel-Aziz; Paola Gratteri; Sahar M. Abou-Seri; Claudiu T. Supuran
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New Spisulosine Derivative promotes robust autophagic response to cancer cells Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-02 Asha Ganesher; Priyank Chaturvedi; Rohit Sahai; Sanjeev Meena; Kalyan Mitra; Dipak Datta; Gautam Panda
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A novel class of small molecule inhibitors with radioprotective properties Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-01 Jan Marek; Ales Tichy; Radim Havelek; Martina Seifrtova; Alzbeta Filipova; Lenka Andrejsova; Tomas Kucera; Lukas Prchal; Lubica Muckova; Martina Rezacova; Zuzana Sinkorova; Jaroslav Pejchal
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Biological evaluation and chemoproteomics reveal potential antibacterial targets of a cajaninstilbene-acid analogue Eur. J. Med. Chem. (IF 4.833) Pub Date : 2020-01-01 Kuo Lu; Wen Hou; Xiao-Fang Xu; Qi Chen; Zhengqiu Li; Jing Lin; Wei-Min Chen
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Diarylamides in anticancer drug discovery: A review of pre-clinical and clinical investigations Eur. J. Med. Chem. (IF 4.833) Pub Date : 2019-12-31 Abduelmula R. Abduelkarem; Hanan S. Anbar; Seyed-Omar Zaraei; Aya A. Alfar; Omayma S. Al-Zoubi; Eveen G. Abdelkarem; Mohammed I. El-Gamal
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Proton pump inhibitors selectively suppress MLL rearranged leukemia cells via disrupting MLL1-WDR5 protein-protein interaction Eur. J. Med. Chem. (IF 4.833) Pub Date : 2019-12-31 Wei-Lin Chen; Dong-Dong Li; Xin Chen; Ying-Zhe Wang; Jun-Jie Xu; Zheng-Yu Jiang; Qi-Dong You; Xiao-Ke Guo
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The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119 Eur. J. Med. Chem. (IF 4.833) Pub Date : 2019-12-31 Gang Li; Bingxu Meng; Baokun Yuan; Yi Huan; Tian Zhou; Qian Jiang; Lei Lei; Li Sheng; Weiping Wang; Ningbo Gong; Yang Lu; Chen Ma; Yan Li; Zhufang Shen; Haihong Huang
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