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Synthesis of 2-guanidinyl pyridines and their trypsin inhibition and docking Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-30 Nahlah Ahmed Al-Hadhrami; Angelique Ladwig; Adeyemi Rahman; Isabel Rozas; J. Paul G. Malthouse; Paul Evans
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An in silico mechanistic insight into HDAC8 activation facilitates the discovery of new small-molecule activators Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-30 Jintong Du; Wen Li; Bo Liu; Yingkai Zhang; Jinming Yu; Xuben Hou; Hao Fang
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An investigative study of antitumor properties of a novel thiazolo[4,5-d]pyrimidine small molecule revealing superior antitumor activity with CDK1 selectivity and potent pro-apoptotic properties Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-07-07 Sameh H. Mohamed; Hossam R. Elgiushy; Heba Taha; Sherif F. Hammad; Nageh A. Abou-Taleb; Khaled A. M. Abouzid; Hussein Sawaf; Zeinab Hassan
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Modulation of TRPV4 and BKCa for treatment of brain diseases Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-30 Na Liu; Fang Yan; Qingjie Ma; Jianhua Zhao
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Synthesis and antibiofilm evaluation of 3-hydroxy-2,3-dihydroquinazolin-4(1H)-one derivatives against opportunistic pathogen Acinetobacter baumannii Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-29 Guo Yang; Cheng Cheng; Guo-Bo Xu; Lei Tang; Kim-Lee Chua; Yuan-Yong Yang
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Design, synthesis and biological evaluation of novel glyoxalase I inhibitors possessing diazenylbenzenesulfonamide moiety as potential anticancer agents Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-07-04 Buthina A. Al-Oudat; Hana'a M. Jaradat; Qosay A. Al-Balas; Nizar A. Al-Shar'i; Amanda Bryant-Friedrich; Mel F. Bedi
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Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL) Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-07-04 Nicole Mayer; Martina Schweiger; Elisabeth Fuchs; Anna K. Migglautsch; Carina Doler; Gernot F. Grabner; Matthias Romauch; Michaela-Christina Melcher; Rudolf Zechner; Robert Zimmermann; Rolf Breinbauer
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Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-07-03 Mei Zhu; Ling Ma; Biao Dong; Guoning Zhang; Juxian Wang; Jinming Zhou; Shan Cen; Yucheng Wang
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4'-C-Aminomethyl-2'-deoxy-2'-fluoroarabinonucleoside increases the nuclease resistance of DNA without inhibiting the ability of a DNA/RNA duplex to activate RNase H Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-30 Tatsuya Tsuchihira; Ryohei Kajino; Yusuke Maeda; Yoshihito Ueno
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Amides as Bioisosteres of Triazole-Based Geranylgeranyl Diphosphate Synthase Inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-30 Daniel B. Goetz; Michelle L. Varney; David F. Wiemer; Sarah A. Holstein
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Junceellolide B, a novel inhibitor of Hepatitis B virus Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-25 Xiaodan Li; Hui Liu; Wei Cheng; Jie Wang; He Zhang; Fengmin Lu; Xiangmei Chen; Wenhan Lin
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Discovery of [1,2,4]triazolo[4,3-a]pyridines as potent Smoothened inhibitors targeting the Hedgehog pathway with improved antitumor activity in vivo Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-15 Nannan Tian; Huanxian Wu; Huiwu Zhang; Danni Yang; Lin Lv; Zichao Yang; Tingting Zhang; Dongling Quan; Lei Zhou; Ying Xie; Yimei Xu; Ning Wei; Jiajie Zhang; Mian Chen; John C. Schmitz; Yuanxin Tian; Shaoyu Wu
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New Coumarin/Sulfocoumarin linked Phenylacrylamides as Selective Transmembrane Carbonic Anhydrase Inhibitors: Synthesis and In-Vitro Biological Evaluation Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-18 Baijayantimala Swain; Andrea Angeli; Priti Singh; Claudiu T. Supuran; Mohammed Arifuddin
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Synthesis of ureido thioglycosides as novel insect β‑N‑acetylhexosaminidase OfHex1 inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-23 Shengqiang Shen; Lili Dong; Huizhe Lu; Yanhong Dong; Qing Yang; Jianjun Zhang
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Structural studies of triazole inhibitors with promising inhibitor effects against antibiotic resistance metallo-β-lactamases Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-18 Zeeshan Muhammad; Susann Skagseth; Marc Boomgaren; Sundus Akhter; Christopher Fröhlich; Aya Ismael; Tony Christopeit; Annette Bayer; Hanna-Kirsti S. Leiros
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Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-17 Taynara L. Silva; Deborah A. dos Santos; Hugo C.R. de Jesus; Dieter Brömme; João B. Fernandes; Marcio W. Paixão; Arlene G. Corrêa; Paulo C. Vieira
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Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-20 Neha Dhiman; Kamalpreet Kaur; Vikas Jaitak
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Design, synthesis and biological activity of novel substituted 3-benzoic acid derivatives as MtDHFR inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-20 Thales Kronenberger; Glaucio Monteiro Ferreira; Alfredo Danilo Ferreira de Souza; Soraya da Silva Santos; Antti Poso; João Augusto Ribeiro; Maurício Temotheo Tavares; Fernando Rogério Pavan; Gustavo Henrique Goulart Trossini; Marcio Vinícius Bertacine Dias; Roberto Parise-Filho
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Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-20 Qifei Li; Jieming Li; Yan Cai; Yuxing Zou; Bin Chen; Feng Zou; Jiaxian Mo; Ting Han; Weiwei Guo; Wenlong Huang; Qianqian Qiu; Hai Qian
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Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-13 Gourav Grover; Rajarshi Nath; Rohit Bhatia; Md Jawaid Akhtar
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Amide derivatives of Gallic acid: Design, synthesis and evaluation of inhibitory activities against in vitro α-synuclein aggregation Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-17 Li Chen; Guo-Long Huang; Ming-Huan Lü; Yun-Xiao Zhang; Ji Xu; Su-Ping Bai
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Design and synthesis of peptide-based chimeric molecules to induce degradation of the estrogen and androgen receptors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-12 Hidetomo Yokoo; Nobumichi Ohoka; Mikihiko Naito; Yosuke Demizu
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Phenyltriazole-functionalized sulfamate inhibitors targeting tyrosyl- or isoleucyl-tRNA synthetase Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-05 Dries De Ruysscher; Luping Pang; Charles-Alexandre Mattelaer; Manesh Nautiyal; Steff De Graef; Jef Rozenski; Sergei V. Strelkov; Eveline Lescrinier; Stephen D. Weeks; Arthur Van Aerschot
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Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT7AR ligands Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-05 Anupam Karki; Hari K. Namballa; Ian Alberts; Wayne W. Harding
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Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl–sulfonyl–phenols Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-04 Konstantinos Koutsopoulos; Vasiliki Lavrentaki; Ioakeim Antoniou; Antonios Kousaxidis; Matina Lefkopoulou; Anna Tsantili-Kakoulidou; Lucia Kovacikova; Milan Stefek; Ioannis Nicolaou
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Synthesis and evaluation of heterocycle structures as potential inhibitors of Mycobacterium tuberculosis UGM. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-02 Carine Maaliki,Jian Fu,Sydney Villaume,Albertus Viljoen,Clément Raynaud,Sokaina Hammoud,Jérôme Thibonnet,Laurent Kremer,Stéphane P Vincent,Emilie Thiery
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Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-06-02 Zhiwen Ye,Chunxia Liu,Feng Zou,Yan Cai,Bin Chen,Yuxing Zou,Jiaxian Mo,Ting Han,Wenlong Huang,Qianqian Qiu,Hai Qian
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Bisphosphonate esters interact with HMG-CoA reductase membrane domain to induce its degradation Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-31 Yosuke Toyota; Hiromasa Yoshioka; Ikuya Sagimori; Yuichi Hashimoto; Kenji Ohgane
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6,6′-Aryl trehalose analogs as potential Mincle ligands Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-31 Omer K. Rasheed; George Ettenger; Cassandra Buhl; Robert Child; Shannon M. Miller; Jay T. Evans; Kendal T. Ryter
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Synthesis and evaluation of 18F labeled crizotinib derivative [18F]FPC as a novel PET probe for imaging c-MET-positive NSCLC tumor Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-30 Qingyu Lin; Yingying Zhang; Zhequan Fu; Bingxin Hu; Zhan Si; Yanzhao Zhao; Hongcheng Shi; Dengfeng Cheng
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Strategies towards potent trypanocidal drugs: Application of Rh-catalyzed [2 + 2 + 2] cycloadditions, sulfonyl phthalide annulation and nitroalkene reactions for the synthesis of substituted quinones and their evaluation against Trypanosoma cruzi Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-30 James M. Wood; Nishikant S. Satam; Renata G. Almeida; Vinicius S. Cristani; Dênis P. de Lima; Luiza Dantas-Pereira; Kelly Salomão; Rubem F.S. Menna-Barreto; Irishi N.N. Namboothiri; John F. Bower; Eufrânio N. da Silva Júnior
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Design, synthesis and evaluation of carbamate-linked uridyl-based inhibitors of human ST6Gal I Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-24 Andrew P. Montgomery; Christopher Dobie; Rémi Szabo; Laura Hallam; Marie Ranson; Haibo Yu; Danielle Skropeta
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Fibroblast growth factor receptor modulators employing diamines with reduced phospholipidosis-inducing potential Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-24 Hiroki Sakai; Hidekazu Inoue; Kenji Murata; Tetsuya Toba; Yoshiari Shimmyo; Nobuhiro Narii; Shin-ya Ueno; Yoshiyuki Igawa; Naohiro Takemoto
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2β-3,4-Unsaturated sialic acid derivatives: synthesis optimization, and biological evaluation as Newcastle disease virus hemagglutinin-neuraminidase inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-24 Paolo La Rocca; Paola Rota; Marco Piccoli; Federica Cirillo; Andrea Ghiroldi; Valentina Franco; Pietro Allevi; Luigi Anastasia
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N1-Substituted benzimidazole scaffold for farnesoid X receptor (FXR) agonists accompanying prominent selectivity against vitamin D receptor (VDR) Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-23 Arisa Masuda; Keigo Gohda; Yusuke Iguchi; Ko Fujimori; Yukiko Yamashita; Keisuke Oda; Mizuho Une; Naoki Teno
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Synthesis and evaluation of new 1-oxa-8-azaspiro[4.5]decane derivatives as candidate radioligands for sigma-1 receptors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-23 Jiale Tian; Yingfang He; Winnie Deuther-Conrad; Hualong Fu; Fang Xie; Ying Zhang; Tao Wang; Xiaojun Zhang; Jinming Zhang; Peter Brust; Yiyun Huang; Hongmei Jia
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Investigation into the influence of an acrylic acid acceptor in organic D-π-A sensitizers against phototoxicity. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-19 Shinichiro Fuse,Wataru Moriya,Shinichi Sato,Hiroyuki Nakamura
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Broad assessment of bioactivity of a collection of spiroindane pyrrolidines through "cell painting". Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-19 Manvendra Singh,Nathan Garza,Zachary Pearson,Justin Douglas,Zarko Boskovic
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Synthesis, cytotoxicity, and in vivo antitumor activity study of parthenolide semicarbazones and thiosemicarbazones. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-19 Xinxin Jia,Qi Liu,Shiyi Wang,Binglin Zeng,Guohua Du,Chen Zhang,Yan Li
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Corrigendum to "A truncated RHAMM protein for discovering novel therapeutic peptides" [Bioorg. Med. Chem. 26 (2018) 5194-5203]. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-16 Alexandra Hauser-Kawaguchi,Cornelia Tolg,Teresa Peart,Mark Milne,Eva A Turley,Leonard G Luyt
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Discovery of N-substituted-3-phenyl-1,6-naphthyridinone derivatives bearing quinoline moiety as selective type II c-Met kinase inhibitors against VEGFR-2. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-12 Hongchuang Xu,Minshu Wang,Fengxu Wu,Linsheng Zhuo,Wei Huang,Nengfang She
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Versatile near-infrared fluorescent probe for in vivo detection of Aβ oligomers. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-12 Fantian Zeng,Jian Yang,Xiaofang Li,Kewen Peng,Chongzhao Ran,Yungen Xu,Yuyan Li
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Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO). Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-12 Anup Patnaik,Laura Axford,Lin Deng,Evan Cohick,Xianglin Ren,Sally Loi,Sam Kecman,Micah Hollis-Symynkywicz,Tyler J Harrison,Julien P N Papillon,Natalie Dales,Lawrence G Hamann,Lac Lee,Jean B Regard,Jovita Marcinkeviciene,Martin L Marro,Andrew W Patterson
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A critical update on the strategies towards modulators targeting androgen receptors. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-12 Hongyu Luan,Pengfei Xu,Ying Meng,Zhiyu Li,Jinlei Bian
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Synthesis of novel 3,5,6-trisubstituted 2-pyridone derivatives and evaluation for their anti-inflammatory activity. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-12 Davana S Gonçalves,Samara M de S Melo,Andrey P Jacomini,Michael J V da Silva,Karlos E Pianoski,Franciele Q Ames,Rafael P Aguiar,Alisson Felipe Oliveira,Hélito Volpato,Danielle L Bidóia,Celso V Nakamura,Ciomar A Bersani-Amado,Davi F Back,Sidnei Moura,Fávero R Paula,Fernanda A Rosa
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Bisbenzylisoquinoline alkaloids and P-glycoprotein function: A structure activity relationship study. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-11 Wencheng Xu,Shuhe Chen,Xiaoqin Wang,Hongguang Wu,Haruki Yamada,Toshihiko Hirano
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Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-11 Xiaoying Jiang,Jianan Guo,Yangjing Lv,Chuansheng Yao,Changjun Zhang,Zhisheng Mi,Yuan Shi,Jinping Gu,Tao Zhou,Renren Bai,Yuanyuan Xie
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Immunomodulation-mediated anticancer activity of a novel compound from Brugmansia suaveolens leaves. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-11 Sunil Kumar,Aditi Gupta,Reena Vohra Saini,Amit Kumar,Kanaya Lal Dhar,Neeraj Mahindroo
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Design, synthesis, and evaluation of a novel macrocyclic anti-EV71 agent. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-08 Peng Li,Siqi Wu,Tianyichen Xiao,Yunlong Li,Zhiming Su,Wei Wei,Fei Hao,Guoping Hu,Fusen Lin,Xinsheng Chen,Zhengxian Gu,Tianwei Lin,Haiying He,Jian Li,Shuhui Chen
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Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-07 Nicholas G. Paciaroni; Verrill M. Norwood; Ranjala Ratnayake; Hendrik Luesch; Robert W. Huigens
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Genetically encoded protein labeling and crosslinking in living Pseudomonas aeruginosa. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-06 Huangtao Zheng,Shixian Lin,Peng R Chen
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Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-06 Lalit K Golani,Farhana Islam,Carrie O'Connor,Aamod S Dekhne,Zhanjun Hou,Larry H Matherly,Aleem Gangjee
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The synthesis and biological evaluation of nucleobases/tetrazole hybrid compounds: A new class of phosphodiesterase type 3 (PDE3) inhibitors. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-05 Mohsen Shekouhy,Somaye Karimian,Ali Moaddeli,Zeinab Faghih,Yousef Delshad,Ali Khalafi-Nezhad
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Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-04 Manoj Patel,B Narasimhulu Naidu,Ira Dicker,Helen Higley,Zeyu Lin,Brian Terry,Tricia Protack,Mark Krystal,Susan Jenkins,Dawn Parker,Chiradeep Panja,Richard Rampulla,Arvind Mathur,Nicholas A Meanwell,Michael A Walker
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Computational-aided design of a library of lactams through a diversity-oriented synthesis strategy. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-04 Fernanda I Saldívar-González,Elena Lenci,Lorenzo Calugi,José L Medina-Franco,Andrea Trabocchi
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Cytosolic delivery of peptidic STAT3 SH2 domain inhibitors. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-05-04 Robert A Cerulli,Livia Shehaj,Isidora Tosic,Kevin Jiang,Jing Wang,David A Frank,Joshua A Kritzer
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Discovery and structure-activity relationships study of positive allosteric modulators of the M3 muscarinic acetylcholine receptor. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-04-30 Hiroaki Tanaka,Kenji Negoro,Takanori Koike,Issei Tsukamoto,Kazuhiro Yokoyama,Jun Maeda,Yusuke Inagaki,Yukinori Shimoshige,Katsutoshi Ino,Kenichiro Ishizu,Taisuke Takahashi
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Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-04-25 Mohammad M Al-Sanea,Ahmed Elkamhawy,Sora Paik,Kyeong Lee,Ahmed M El Kerdawy,Bukhari Syed Nasir Abbas,Eun Joo Roh,Wagdy M Eldehna,Heba A H Elshemy,Rania B Bakr,Ibrahim Ali Farahat,Abdulaziz I Alzarea,Sami I Alzarea,Khalid S Alharbi,Mohamed A Abdelgawad
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Exploring tryptamine conjugates as pronucleotides of phosphate-modified 7-methylguanine nucleotides targeting cap-dependent translation. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-04-25 Sebastian Golojuch,Michal Kopcial,Dominika Strzelecka,Renata Kasprzyk,Natalia Baran,Pawel J Sikorski,Joanna Kowalska,Jacek Jemielity
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Synthesis and biological evaluation of triazolyl-substituted benzyloxyacetohydroxamic acids as LpxC inhibitors. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-04-25 Katharina Hoff,Sebastian Mielniczuk,Oriana Agoglitta,Maria Teresa Iorio,Manlio Caldara,Emre F Bülbül,Jelena Melesina,Wolfgang Sippl,Ralph Holl
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