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Multicomponent reactions in crop protection chemistry Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-31 Clemens Lamberth
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Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer’s disease: radical scavenging, Myeloperoxidase/Acetylcholinesterase inhibition and Biometal chelation Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-31 Daniela Corrêa Santos; Ruan Roberto Henriques; Marcos Antonio de Abreu Lopes Junior; André Borges Farias; Thayssa Lisboa do Couto Nogueira; João Victor Fernandes Quimas; Nelilma Correia Romeiro; Leandro Louback da Silva; Andréa Luzia Ferreira de Souza
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Design and Optimization of a Series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual Inhibitors of TYK2 and JAK1 Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-31 Andrew Fensome; Catherine M. Ambler; Eric Arnold; Mary Ellen Banker; James D. Clark; Martin E. Dowty; Ivan V. Efremov; Andrew Flick; Brian S. Gerstenberger; Roger S. Gifford; Ariamala Gopalsamy; Martin Hegen; Jason Jussif; David C. Limburg; Tsung H. Lin; Betsy S. Pierce; Raman Sharma; John I. Trujillo; Xin Yang
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Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-31 Malikotsi A. Qhobosheane; Lesetja J. Legoabe; Béatrice Josselin; Stéphane Bach; Sandrine Ruchaud; Jacobus P. Petzer; Richard M. Beteck
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Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-29 Przemysław Zaręba; Anna K. Drabczyk; Jolanta Jaśkowska; Grzegorz Satała
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Microbial transformation of glycyrrhetinic acid derivatives by Bacillus subtilis ATCC 6633 and Bacillus megaterium CGMCC 1.1741 Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-29 Ping-ping Shen; Jian Zhang; Yu-yuan Zhu; Wei Wang; Bo-yang Yu; Wei-wei Wang
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Characterization of alditol oxidase from Streptomyces coelicolor and its application in the production of rare sugars Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-29 Zhou Chen; Zijie Li; Fen Li; Ning Wang; Xiao-Dong Gao
A synthetic platform for the cascade synthesis of rare sugars using Escherichia coli whole cells was established. In the cascade, the donor substrate dihydroxyacetone phosphate (DHAP) was generated from the starting material glycerol by glycerol kinase (GK) and glycerol phosphate oxidase (GPO). The acceptor D-glyceraldehyde was directly produced from glycerol by alditol oxidase. Then, the aldol reaction
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Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-28 Krishnappa Ramya; Ramalingam Suresh; Honnavalli Yogish Kumar; B.R. Prashantha Kumar; N.B. Sridhara Murthy
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Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2 Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-28 Ikumi Kuriwaki; Minoru Kameda; Hiroyuki Hisamichi; Shigetoshi Kikuchi; Kazuhiko Iikubo; Yuichiro Kawamoto; Hiroyuki Moritomo; Yutaka Kondoh; Yasushi Amano; Yukihiro Tateishi; Yuka Echizen; Yoshinori Iwai; Atsushi Noda; Hiroshi Tomiyama; Tomoyuki Suzuki; Masaaki Hirano
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New CDK8 inhibitors as potential anti-leukemic agents – design, synthesis and biological evaluation Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-27 Eirik J. Solum; Trond Vidar Hansen; Reidun Aesoy; Lars Herfindal
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α-Glucosidase inhibitory and nitric oxide production inhibitory activities of alkaloids isolated from a twig extract of Polyalthia cinnamomea Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-27 Virayu Suthiphasilp; Wisanu Maneerat; Narawadee Rujanapun; Thidarat Duangyod; Rawiwan Charoensup; Suwanna Deachathai; Raymond J. Andersen; Brian O. Patrick; Stephen G. Pyne; Surat Laphookhieo
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PNA-Based Dynamic Combinatorial libraries (PDCL) and screening of lectins Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-26 Lluc Farrera-Soler; Jean-Pierre Daguer; Patrick Raunft; Sofia Barluenga; Anne Imberty; Nicolas Winssinger
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Antifungal polyketide derivatives from the endophytic fungus Aplosporella javeedii Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-25 Ying Gao; Lin Wang; Rainer Kalscheuer; Zhen Liu; Peter Proksch
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Chemical reactivity and uses of 1-phenyl-3-methyl-5-pyrazolone (PMP), also known as edaravone Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-25 Christian Bailly; Paul-Emile Hecquet; Mostafa Kouach; Xavier Thuru; Jean-François Goossens
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Needle in a haystack: Antibacterial activity-guided fractionation of a potato wound tissue extract Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-23 Mathiu Perez Rodriguez; Keyvan Dastmalchi; Barney Yoo; Ruth E. Stark
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Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for γ-secretase modulators with oral efficacy against cognitive deficits in Alzheimer’s disease model mice Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-22 Ryuichi Sekioka; Shugo Honda; Hiroki Akashiba; Junko Yarimizu; Yasuyuki Mitani; Shingo Yamasaki
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A chemically stable peptide agonist to neuromedin U receptor type 2 Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-22 Kentaro Takayama; Kenji Mori; Akiko Tanaka; Yu Sasaki; Yuko Sohma; Akihiro Taguchi; Atsuhiko Taniguchi; Toshiyasu Sakane; Akira Yamamoto; Mikiya Miyazato; Naoto Minamino; Kenji Kangawa; Yoshio Hayashi
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Anti-inflammatory effect and inhibition of nitric oxide production by targeting COXs and iNOS enzymes with the 1,2-diphenylbenzimidazole pharmacophore Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-21 Mónica I. García-Aranda; Jazmin E. Gonzalez-Padilla; Carlos Z. Gómez-Castro; Yolanda M. Gómez-Gómez; Martha C. Rosales-Hernández; Efrén V. García-Báez; Marina O. Franco-Hernández; José L. Castrejón-Flores; Itzia I. Padilla-Martínez
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Identification and in silico prediction of metabolites of tebufenozide derivatives by major human cytochrome P450 isoforms Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-19 Hiroaki Edamatsu; Masataka Yagawa; Shinichi Ikushiro; Toshiyuki Sakaki; Yoshiaki Nakagawa; Hisashi Miyagawa; Miki Akamatsu
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Synthesis, biological evaluation and virtual screening of some acridone derivatives as potential anticancer agents Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-19 Abiodun S. Oyedele; Deanna N. Bogan; Cosmas O. Okoro
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A Novel Potent Metal-binding NDM-1 Inhibitor was Identified by Fragment Virtual, SPR and NMR Screening Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-18 Huifang Guo; Kai Cheng; Yan Gao; Weiqi Bai; Cai Wu; Wei He; Conggang Li; Zhuorong Li
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New acrylamide-sulfisoxazole conjugates as dihydropteroate synthase inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-18 Tamer Nasr; Samir Bondock; Tamer M. Ibrahim; Walid Fayad; Ahmed B. Ibrahim; Neveen A. AbdelAziz; Tamer M. Sakr
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Fluorescence detection of the nitric oxide-induced structural change at the putative nitric oxide sensing segment of TRPC5 Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-17 Shunsuke Tajima; Eiji Nakata; Reiko Sakaguchi; Masayuki Saimura; Yasuo Mori; Takashi Morii
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Translation of the copper/bipyridine-promoted Petasis reaction to solid phase-coupled DNA for encoded library synthesis Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-17 Marco Potowski; Robin Esken; Andreas Brunschweiger
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Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-17 Maria Rosa Buemi; Rosaria Gitto; Laura Ielo; Christophe Pannecouque; Laura De Luca
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Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-17 Babita Aneja; Aarfa Queen; Parvez Khan; Farheen Shamsi; Afzal Hussain; Phool Hasan; M. Moshahid A. Rizvi; Constantin G. Daniliuc; Mohamed F. Alajmi; Mohd. Mohsin; Md. Imtaiyaz Hassan; Mohammad Abid
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Synthesis and biological evaluation of new antioxidant and antiproliferative chalcogenobiotin derivatives for bladder carcinoma treatment Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-16 Andrielli Leitemberger; Mariana S. Sonego; Fábio D. Garcia; Alana C.F. dos Santos; Bruna C. Piccoli; Fernanda D. da Silva; Cláudia S. Oliveira; Fabiana K. Seixas; Luciano Dornelles; João B.T. Rocha; Pablo A. Nogara; Kyle M. Schachtschneider; Tiago Collares; Oscar E.D. Rodrigues
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A-Ring and E-Ring Modifications of the Cytotoxic Alkaloid Luotonin A: Synthesis, Computational and Biological Studies Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-16 Amra Ibric; Verena Battisti; Sophie Deckardt; Anna Veronika Haller; Calvin Lee; Corinna Prötsch; Thierry Langer; Petra Heffeter; Hemma Henrike Schueffl; Brigitte Marian; Norbert Haider
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Synthesis and Evaluation of the Performance of a Small Molecule Library Based on Diverse Tropane-Related Scaffolds Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-16 Robert A. Lowe; Dale Taylor; Kelly Chibale; Adam Nelson; Stephen P. Marsden
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High Throughput in vivo Phenotypic Screening for Drug Repurposing: Discovery of MLR-1023 a Novel insulin Sensitizer and Novel Lyn Kinase Activator with Clinical Proof of Concept Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-16 Christopher A. Lipinski; Andrew G. Reaume
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Structural motives controlling the binding affinity of 9,10-bis(methylpyridinium)anthracenes towards DNA Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-16 Werner Fudickar; Torsten Linker
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Synthesis of Novel Dual Target Inhibitors of PARP and HSP90 and Their Antitumor Activities Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-13 Shanshan Lin; LingYu Zhang; Xiao Zhang; Zelei Yu; Xiuwang Huang; Jianhua Xu; Yang Liu; Limin Chen; Lixian Wu
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Identification of an ethyl 5,6-dihydropyrazolo[1,5-c]quinazoline-1-carboxylate as a catalytic inhibitor of DNA gyrase Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-13 Arturo L. Aguirre; Pratik R. Chheda; Sarah R.C. Lentz; Hailey A. Held; Natalie P. Groves; Hiroshi Hiasa; Robert J. Kerns
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Structure-based Design and Synthesis of Novel Furan-Diketopiperazine-Type Derivatives as Potent Microtubule Inhibitors for Treating Cancer Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-13 Zhongpeng Ding; Feifei Li; Changjiang Zhong; Feng Li; Yuqian Liu; Shixiao Wang; Jianchun Zhao; Wenbao Li
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Identification and Synthesis of an Efficient Multivalent E. coli Heat Labile Toxin Inhibitor __ A Dynamic Combinatorial Chemistry Approach Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-13 Jintao Xu; Shixin Zhang; Shuang Zhao; Lei Hu
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Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-13 Long Zhao; Keyao Luo; Zhaojuan Wang; Yuan Wang; Xianghui Zhang; Dongxu Yang; Mengtao Ma; Jingjing Zhou; Jiaming Cui; Jing Wang; Chao-zhen-yi Han; Xin Liu; Rui Wang
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Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-13 Isaac O. Donkor; Jin Xu; Jiuyu Liu; Keyuna Cameron
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Predictive Models For Estimating Cytotoxicity On The Basis Of Chemical Structures Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-12 Hongmao Sun; Yuhong Wang; Dorian M. Cheff; Matthew D. Hall; Min Shen
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Small molecule inhibitors of IκB kinase β: a chip-based screening and molecular docking simulation Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-12 Yong Wan Cho; Hye Jin Lim; Moon Hi Han; Byung-Chul Kim; Sanghwa Han
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Investigations of Antiproliferative and Antioxidant Activity of β-Lactam Morpholino-1,3,5-Triazine Hybrids Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-04 Somayeh Ranjbari; Maryam Behzadi; Saghi Sepehri; Marzieh Dadkhah Aseman; Aliasghar Jarrahpour; Milad Mohkam; Younes Ghasemi; Amin Reza Akbarizadeh; Sedigheh Kianpour; Zeliha Atioğlu; Namık Özdemir; Mehmet Akkurt; S. Masoud Nabavizadeh; Edward Turos
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Chemical Synthesis and Properties of Modified Oligonucleotides Containing 5′-Amino-5′-deoxy-5′-hydroxymethylthymidine Residues Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-03 Akihiro Ohkubo; Kousuke Muto; Rintaro Watanabe; Shuhei Nishizawa; Shugo Hisamatsu; Takashi Kanamori
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Interruption of Vif/Elongin C interaction: In silico and experimental elucidation of the underlying molecular mechanism of benzimidazole-based APOBEC3G stabilizers Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-03 Mohamed O. Radwan; Daisuke Takaya; Ryoko Koga; Kana Iwamaru; Hiroshi Tateishi; Taha F.S. Ali; Akifumi Takaori-Kondo; Masami Otsuka; Teruki Honma; Mikako Fujita
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Drug repurposing and rediscovery: Design, synthesis and preliminary biological evaluation of 1-arylamino-3-aryloxypropan-2-ols as anti-melanoma agents Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-03 Qi Chang; Jing Long; Liqing Hu; Zhuo Chen; Qianbin Li; Gaoyun Hu
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A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-03 Mohammed I. El-Gamal; Seyed-Omar Zaraei; Paul A. Foster; Hanan S. Anbar; Randa El-Gamal; Raafat El-Awady; Barry V.L. Potter
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Double-component diazeniumdiolate derivatives as anti-cancer agents Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-03-03 Xun Ji; Qi Chen; Viswanath Arutla; Omar Khdour; Qiong-Ying Hu; Shengxi Chen
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Rational modifications, synthesis and biological evaluation of new potential antivirals for RSV designed to target the M2-1 protein. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-26 Salvatore Ferla,Roberto Manganaro,Sara Benato,Jasmine Paulissen,Johan Neyts,Dirk Jochmans,Andrea Brancale,Marcella Bassetto
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Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-26 Mohammed T-E Maghraby,Ola M F Abou-Ghadir,Samia G Abdel-Moty,Asmaa Y Ali,Ola I A Salem
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Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-26 Li Luo; Qing Song; Yan Li; Zhongcheng Cao; Xiaoming Qiang; Zhenghuai Tan; Yong Deng
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siRNA delivery using amphipathic cell-penetrating peptides into human hepatoma cells Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-25 Kaori Furukawa; Masakazu Tanaka; Makoto Oba
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Promising antifungal agents: A minireview. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-21 K V S Mani Chandrika,Sahida Sharma
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Bifunctional small molecule-oligonucleotide hybrid as microRNA inhibitor Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-18 Umesh Bhattarai; Wei-Che Hsieh; Hao Yan; Zhi-Fo Guo; Ashif Yasin Shaikh; Aria Soltani; Yabin Song; Danith H. Ly; Fu-Sen Liang
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Ligand-based design of GLUT inhibitors as potential antitumor agents. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-18 Suliman Almahmoud,Wei Jin,Liying Geng,Jing Wang,Xiaofang Wang,Jonathan L Vennerstrom,Haizhen A Zhong
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Carcinogenic roles and therapeutic effects of EZH2 in gynecological cancers. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-17 Zhong Wan,Huabo Jiang,Li Li,Shuhui Zhu,Jingjing Hou,Yongsheng Yu
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Synthesis, biological evaluation and molecular modeling study of [1,2,4]-Triazolo[4,3-c]quinazolines: New class of EGFR-TK inhibitors. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-13 Wafaa A Ewes,Mohammad A Elmorsy,Shahenda M El-Messery,Magda N A Nasr
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Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-13 Ziyi Yang,Qing Song,Zhongcheng Cao,Guangjun Yu,Zhuoling Liu,Zhenghuai Tan,Yong Deng
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DNA sequence-specific ligands. XVIII. Synthesis, physico-chemical properties; genetic, virological, and biochemical studies of fluorescent dimeric bisbenzimidazoles DBPA(n). Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-13 Vasiliy S Koval,Albert F Arutyunyan,Victor I Salyanov,Alexey A Kostyukov,Olga E Melkina,Gennadii B Zavilgelsky,Regina R Klimova,Alla A Kushch,Sergey P Korolev,Yulia Yu Agapkina,Marina B Gottikh,Andrey V Vaiman,Ekaterina Yu Rybalkina,Olga Yu Susova,Alexei L Zhuze
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Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-13 Wenjian Min,Zeng Hou,Fang Zhang,Shengnan Xie,Kai Yuan,Haojie Dong,Liping Wang,Lianwen Qi,Cheng Luo,Hong Ding,Peng Yang
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Enhanced cellular uptake efficiency of DCM probes or SN38 conjugating with phenylboronic acids. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-17 Qiumeng Zhang,Rui Che,Wei Lu
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Selective modification of alkyne-linked peptides and proteins by cyclometalated gold(III) (C^N) complex-mediated alkynylation. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-28 Hok-Ming Ko,Jie-Ren Deng,Jian-Fang Cui,Karen Ka-Yan Kung,Yun-Chung Leung,Man-Kin Wong
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Discovery of 1,8-naphthyridin-2-one derivative as a potent and selective sphingomyelin synthase 2 inhibitor. Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-02-12 Takafumi Yukawa,Takashi Nakahata,Rei Okamoto,Yuji Ishichi,Yasufumi Miyamoto,Satoshi Nishimura,Tatsuo Oikawa,Kazuki Kubo,Ryutaro Adachi,Yoshinori Satomi,Masanori Nakakariya,Nobuyuki Amano,Masahiro Kamaura,Nobuyuki Matsunaga
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