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Substituted pteridinones as p90 ribosomal S6 protein kinase (RSK) inhibitors: a structure-activity study Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-12 Kimberly A. Casalvieri; Christopher J. Matheson; Donald S. Backos; Philip Reigan
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Relationship Among Structure, Cytotoxicity, and Michael Acceptor Reactivity of Quinocidin Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-11 Yu Nakagawa; Yuki Sawaki; Wataru Miyanishi; Sayako Shimomura; Takahiro Shibata; Makoto Ojika
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A selective and sensitive turn-on chemosensor for detection of Fe3+ in aqueous solution and its cell imaging in Dorsal root ganglia neurons and MKN-45 cells Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-10 Yangyan Qian; Jinshuai Suo; Zhigang Gao; Haibo Liu; Qinghan Hua; Yuting Lu; Peng Zhang; Chun Kan; Xiaofeng Bao; Jing Zhu
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Phosphine boranes as less hydrophobic building blocks than alkanes and silanes: structure-property relationship and estrogen-receptor-modulating potency of 4-phosphinophenol derivatives Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-09 Hiroki Saito; Yuichiro Matsumoto; Yuichi Hashimoto; Shinya Fujii
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Development of a Potent and Orally Active Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), ASP4132, as a Clinical Candidate for the Treatment of Human Cancer Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-08 Kazuyuki Kuramoto; Hiroyoshi Yamada; Takashi Shin; Yuki Sawada; Hidenori Azami; Tomohiro Yamada; Takeyuki Nagashima; Kei Ohnuki
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Targeting the DNA damage response (DDR) by natural compounds Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-08 Jana van Stuijvenberg; Peter Proksch; Gerhard Fritz
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Anti-diabetic drugs recent approaches and advancements Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-08 Jayanta Dowarah; Ved Prakash Singh
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Cytotoxic and non-cytotoxic cardiac glycosides isolated from the combined flowers, leaves, and twigs of Streblus asper Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-07 Yulin Ren; Qingwei Tan; Kimberly Heath; Sijin Wu; James R. Wilson; Jinhong Ren; Pratik Shriwas; Chunhua Yuan; Tran Ngoc Ninh; Hee-Byung Chai; Xiaozhuo Chen; Djaja D. Soejarto; Michael E. Johnson; Xiaolin Cheng; Joanna E. Burdette; A. Douglas Kinghorn
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New modification strategy of matrine as Hsp90 inhibitors based on its specific L conformation for cancer treatment Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-07 Yiming Xu; Dewang Jing; Dong Zhao; Yongji Wu; Lu Xing; Haroon ur Rashid; Haodong Wang; Lisheng Wang; Huiling Cao
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PEGylated Leuprolide with Improved Pharmacokinetic Properties Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-07 Mian Fu; Xiaomei Zhuang; Tianhong Zhang; Ying Guan; Qingbin Meng; Yongjun Zhang
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Mangiferin: a promising natural xanthone from Mangifera indica for the control of acyclovir – resistant herpes simplex virus 1 infection Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-07 Daniele Zendrini Rechenchoski; Karoline Fontana Agostinho; Ligia Carla Faccin-Galhardi; Audrey Alesandra Stinghen Garcia Lonni; João Vinícius Honório da Silva; Fábio Goulart de Andrade; Arcelina Pacheco Cunha; Nágila Maria Pontes Silva Ricardo; Carlos Nozawa; Rosa Elisa Carvalho Linhares
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New compounds for a good old class: synthesis of two Β-lactam bearing cephalosporins and their evaluation with a multidisciplinary approach Bioorg. Med. Chem. (IF 2.802) Pub Date : 2020-01-03 Giovanni Vigliotta; Deborah Giordano; Anna Verdino; Ivana Caputo; Stefania Martucciello; Annunziata Soriente; Anna Marabotti; Margherita De Rosa
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Comparing a Thioglycosylated Chlorin and Phthalocyanine as Potential Theranostic Agents Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-30 Sunaina Singh; Amit Aggarwal; N.V.S. Dinesh K. Bhupathiraju; Ivana Radivojevic Jovanovic; Michael Landress; Michelle Paola Tuz; Ruomei Gao; Charles M. Drain
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N-(3,5-Dichloro-4-(2,4,6-trichlorophenoxy)phenyl)benzenesulfonamide: A new dual-target inhibitor of mitochondrial complex II and complex III via structural simplification Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-30 Hua Cheng; Hong-Fu Liu; Lu Yang; Cheng Chen; Yuan Wu; Wen Jiang; Rui Zhang
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Evaluation of an octahydroisochromene scaffold used as a novel SARS 3CL protease inhibitor Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-30 Shin-ichiro Yoshizawa; Yasunao Hattori; Kazuya Kobayashi; Kenichi Akaji
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3D proteome-wide scale screening and activity evaluation of a new ALKBH5 inhibitor in U87 glioblastoma cell line Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-30 Alessio Malacrida; Mirko Rivara; Alessandro Di Domizio; Giacomo Cislaghi; Mariarosaria Miloso; Valentina Zuliani; Gabriella Nicolini
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Luciferase-based HMG-CoA reductase degradation assay for activity and selectivity profiling of oxy(lano)sterols Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-30 Ikuya Sagimori; Hiromasa Yoshioka; Yuichi Hashimoto; Kenji Ohgane
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Impact of the structure-activity relationship of AHL analogues on quorum sensing in Gram- negative bacteria Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-28 Christiane Chbib
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Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-26 Haoquan He; Zheng Liu; Wei Wang; Xiaojian Jiang
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Optimisation of Estrogen Receptor Subtype-Selectivity of a 4-Aryl-4H-Chromene Scaffold Previously Identified by Virtual Screening Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-24 Miriam Carr; Andrew J.S. Knox; Daniel K. Nevin; Niamh O'Boyle; Shu Wang; Billy Egan; Thomas McCabe; Brendan Twamley; Daniela M. Zisterer; David G. Lloyd; Mary J. Meegan
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A novel fluorescent probe based on naphthalimide for imaging nitroreductase (NTR) in bacteria and cells Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-24 Zijian Zhang; Ting Lv; Binbin Tao; Zhenfu Wen; Yongqian Xu; Hongjuan Li; Fengyu Liu; Shiguo Sun
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Synthesis and Biological Evaluation of 2-Quinolineacrylamides Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-19 Shih-Wei Wang; Mei-Hsiang Lin; Fu-Chun Hsu; Mei-Chuan Chen; Jing-Ping Liou; Yi-Ting Liu; Shiou-Sheng Chen; Hsueh-Yun Lee
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In Situ Localization of Alkaline Phosphatase Activity in Tumor Cells by an Aggregation-Induced Emission Fluorophore-Based Probes Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-19 Qinghua Guan; Xinmiao Lu; Yue Su; Jichen Xu; Xiaofei Liang; Peiyong Li; Xinyuan Zhu
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miR-140-3p impedes the proliferation of human cervical cancer cells by targeting RRM2 to induce cell-cycle arrest and early apoptosis Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-19 Jiajia Ma; Fan Zhang; Ping Sun
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Expanding therapeutic opportunities for neurodegenerative diseases: A perspective on the important role of phenotypic screening Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-18 Susanne E. Swalley
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Molecular mechanism of C-phycocyanin induced apoptosis in LNCaP cells Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-18 Paramjot Kaur; Sivanesan Dhandayuthapani; Thiagarajan Venkatesan; Miroslav Gantor; Appu Rathinavelu
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Bisphenol AF: Halogen bonding effect is a major driving force for the dual ERα-agonist and ERβ-antagonist activities Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-18 Xiaohui Liu; Keitaro Suyama; Junichi Shiki; Kohei Torikai; Takeru Nose; Miki Shimohigashi; Yasuyuki Shimohigashi
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Synthesis and Biological Activity of Thieno[3,2-d]pyrimidines as Potent JAK3 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-14 Yanming Zhu; Xu Zheng; Changyuan Wang; Xiuli Sun; Huijun Sun; Tengyue Ma; Yanxia Li; Kexin Liu; Lixue Chen; Xiaodong Ma
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Formaldehyde-activated WEHI-150 induces DNA interstrand crosslinks with unique structural features Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-14 Paul P. Pumuye; Benny J. Evison; Shyam K. Konda; J. Grant Collins; Celine Kelso; Jelena Medan; Brad E. Sleebs; Keith Watson; Don R. Phillips; Suzanne M. Cutts
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Synthesis, biological evaluation and anti-proliferative mechanism of fluorine-containing proguanil derivatives Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-12 Di Xiao; Zhicheng Lu; Zhiren Wang; Sichun Zhou; Mengru Cao; Jun Deng; Xin Hu; Mei Peng; Caimei He; Jintao Wu; Simeng Xu; Huihui Zhang; Cangcang Xu; Wei Wang; Aiying Guan; Xiaoping Yang
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Synthesis of novel 5-substituted-2-aminotetralin analogs: 5-HT1A and 5-HT7 G protein-coupled receptor affinity, 3D-QSAR and molecular modeling Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-12 Charles K. Perry; Austen B. Casey; Daniel E. Felsing; Rajender Vemula; Mehreen Zaka; Noah B. Herrington; Meng Cui; Glen E. Kellogg; Clinton E. Canal; Raymond G. Booth
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Heteroarylamide Smoothened Inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254) Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-11 Bin Yang, Alexander W. Hird, Michael S. Bodnarchuk, Xiaolan Zheng, Les Dakin, Qibin Su, Kevin Daly, Robert Godin, Maureen M. Hattersley, Patrick Brassil, Sean Redmond, Daniel John Russell, James W. Janetka
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Identification of vibsanin A analog as a novel HSP90 inhibitor Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-09 Kazuki Miura, Wataru Matsuki, Akihiro Ogura, Ken-ichi Takao, Siro Simizu
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Bilobalide and PC12 Cells: A Structure Activity Relationship Study Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-09 Toyonobu Usuki, Yukiko Yoshimoto, Makiko Sato, Tae Takenaka, Ryota Takezawa, Yusuke Yoshida, Masayuki Satake, Noriyuki Suzuki, Daisuke Hashizume, Sergei V. Dzyuba
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Synthesis of novel 2-pyrrolidinone and pyrrolidine derivatives and study of their inhibitory activity against autotaxin enzyme Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-09 Dimitrios Triantafyllos Gerokonstantis, Aikaterini Nikolaou, Christiana Magkrioti, Antreas Afantitis, Vassilis Aidinis, George Kokotos, Panagiota Moutevelis-Minakakis
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Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-09 Antonio Laghezza, Grazia Luisi, Alessia Caradonna, Antonella Di Pizio, Luca Piemontese, Fulvio Loiodice, Mariangela Agamennone, Paolo Tortorella
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Identification of Mycobacterium tuberculosis CtpF as a target for designing new antituberculous compounds Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-09 Paola Santos, Fabian Lopez-Vallejo, David Ramírez, Julio Caballero, Dulce Mata Espinosa, Rogelio Hernández-Pando, Carlos Y. Soto
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Discovery of 1,2,4-oxadiazole derivatives as a novel class of noncompetitive inhibitors of 3-hydroxykynurenine transaminase (HKT) from Aedes aegypti Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-09 Larissa G. Maciel, Andrew A. Oliveira, Tatiany P. Romão, Laylla L.L. Leal, Rafael V.C. Guido, Maria Helena N.L. Silva-Filha, Janaína V. dos Anjos, Thereza A. Soares
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Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-09 Sören Baumeister, Dirk Schepmann, Bernhard Wünsch
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Structural insights into the active site of poly(ADP-ribose) glycohydrolase using docking modes of 6-hydroxy-3H-xanthen-3-one derivative inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-06 Yuto Shibui, Takahiro Oyama, Miwa Okazawa, Atsushi Yoshimori, Hideaki Abe, Fumiaki Uchiumi, Sei-ichi Tanuma
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Targeted suppression of metastasis regulatory transcription factor SOX2 in various cancer cell lines using a sequence-specific designer pyrrole–imidazole polyamide Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-06 Madhu Malinee, Alok Kumar, Takuya Hidaka, Masanobu Horie, Kouichi Hasegawa, Ganesh N. Pandian, Hiroshi Sugiyama
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Modification of the Lead Molecule: Tryptophan and Piperidine Appended Triazines Reversing Inflammation and Hyeperalgesia in Rats Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-06 Priya Kumari, Sukhmeet Kaur, Jashanpreet Kaur, Rajbir Bhatti, Palwinder Singh
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Auxiliary in vitro and in vivo biological evaluation of hydrogen peroxide sensitive prodrugs of methotrexate and aminopterin for the treatment of rheumatoid arthritis Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-06 Viola Previtali, Katarina Petrovic, Jorge Peiró Cadahía, Nikolaj Sten Troelsen, Mads H. Clausen
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Discovery and Preclinical Development of AR453588 as an Anti-diabetic Glucokinase Activator Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-02 Ronald J. Hinklin, Brian R. Baer, Steven A. Boyd, Mark D. Chicarelli, Kevin R. Condroski, Walter E. DeWolf, John Fischer, Michele Frank, Gary P. Hingorani, Patrice A. Lee, Nickolas A. Neitzel, Scott A. Pratt, Ajay Singh, Francis X. Sullivan, Timothy Turner, Walter C. Voegtli, Eli M. Wallace, Lance Williams, Thomas D. Aicher
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Recent advances in the discovery and development of glyoxalase I inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-02 Tian Jin, Lu Zhao, Hong-Ping Wang, Mao-Lin Huang, Yan Yue, Chichong Lu, Zhe-Bin Zheng
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Tetrahydroquinoline units in flexible heteroarotinoids (Flex-Hets) convey anti-cancer properties in A2780 ovarian cancer cells Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-02 Krishna Kumar Gnanasekaran, Tim Pouland, Richard A. Bunce, K. Darrell Berlin, Suaad Abuskhuna, Dipendra Bhandari, Maryam Mashayekhi, Donghua H. Zhou, Doris M. Benbrook
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A novel phytosterol isolated from Datura inoxia, RinoxiaB is a potential cure colon cancer agent by targeting BAX/Bcl2 pathway Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-12-02 Babu Gajendran, Prabhu Durai, Krishnapriya Madhu Varier, Arulvasu Chinnasamy
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Exploring Structure-Promiscuity Relationships Using Dual-Site Promiscuity Cliffs and Corresponding Single-Site Analogs Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Huabin Hu, Jürgen Bajorath
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A scaffold replacement approach towards new sirtuin 2 inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Tina Seifert, Marcus Malo, Tarja Kokkola, E. Johanna L. Stéen, Kristian Meinander, Erik A.A. Wallén, Elina M. Jarho, Kristina Luthman
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Identification of novel inhibitors for the tyrosyl-DNA-phosphodiesterase 1 (Tdp1) mutant SCAN1 using virtual screening Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 E.M. Mamontova, A.L. Zakharenko, O.D. Zakharova, N.S. Dyrkheeva, K.P. Volcho, J. Reynisson, H.J. Arabshahi, N.F. Salakhutdinov, O.I. Lavrik
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Design and Synthesis of Boron-containing Diphenylpyrimidines as Potent BTK and JAK3 Dual Inhibitors Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Jing Ren, Wei Shi, Damin Zhao, Qinglin Wang, Xiayun Chang, Xiangyi He, Xiaojin Wang, Yong Gao, Peng Lu, Xiquan Zhang, Hongjiang Xu, Yinsheng Zhang
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A benzenesulfonamide derivative as a novel PET radioligand for CXCR4 Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Yoon Hyeun Oum, Dinesh Shetty, Younghyoun Yoon, Zhongxing Liang, Ronald J. Voll, Mark M. Goodman, Hyunsuk Shim
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Lipidated α/Sulfono-α-AA heterogeneous peptides as antimicrobial agents for MRSA Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Sylvia Singh, Minghui Wang, Ruixuan Gao, Peng Teng, Timothy Odom, En Zhang, Hai Xu, Jianfeng Cai
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Metachromins X and Y from a marine sponge Spongia sp. and their effects on cell cycle progression Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Yuki Hitora, Kentaro Takada, Yuji Ise, Sau Pinn Woo, Seiya Inoue, Naoki Mori, Hirosato Takikawa, Shohei Nakamukai, Shigeru Okada, Shigeki Matsunaga
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Identification of Potent Pyrazole Based APELIN Receptor (APJ) Agonists Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Sanju Narayanan, Vineetha Vasukuttan, Sudarshan Rajagopal, Rangan Maitra, Scott P. Runyon
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Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-30 Fangqing Zhang, Zhenwei Wu, Pan Chen, Jian Zhang, Tao Wang, Jinpei Zhou, Huibin Zhang
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Small Molecules Targeting HIF-1α Pathway for Cancer Therapy in Recent Years Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-29 Wendi Tang, Guisen Zhao
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New aromatic 6-substituted 2́-deoxy-9-(β)-d-ribofuranosylpurine derivatives as potential plant growth regulators Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-29 Vlasta Matušková, Marek Zatloukal, Jiří Voller, Jiří Grúz, Zuzana Pěkná, Katarína Briestenská, Jela Mistríková, Lukáš Spíchal, Karel Doležal, Miroslav Strnad
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Identification of small-molecule urea derivatives as novel NAMPT inhibitors via pharmacophore-based virtual screening Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-29 Fikriye Ozgencil, Gokcen Eren, Yesim Ozkan, Sezen Guntekin-Ergun, Rengul Cetin-Atalay
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Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ Bioorg. Med. Chem. (IF 2.802) Pub Date : 2019-11-28 Seungchan An, Jinha Yu, Hongseok Choi, Hyejin Ko, Sungjin Ahn, Jeayoung C. Shin, Jeong Joo Pyo, Lak Shin Jeong, Minsoo Noh
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