Literature DB >> 22727640

Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.

Les A Dakin1, Michael H Block, Huawei Chen, Erin Code, James E Dowling, Xiaomei Feng, Andrew D Ferguson, Isabelle Green, Alexander W Hird, Tina Howard, Erika K Keeton, Michelle L Lamb, Paul D Lyne, Hannah Pollard, Jon Read, Allan J Wu, Tao Zhang, Xiaolan Zheng.   

Abstract

Novel substituted benzylidene-1,3-thiazolidine-2,4-diones (TZDs) have been identified as potent and highly selective inhibitors of the PIM kinases. The synthesis and SAR of these compounds are described, along with X-ray crystallographic, anti-proliferative, and selectivity data.
Copyright © 2012. Published by Elsevier Ltd.

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Year:  2012        PMID： 22727640     DOI： 10.1016/j.bmcl.2012.05.098

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  21 in total

1.  Design and Synthesis of Potent and Selective PIM Kinase Inhibitors by Targeting Unique Structure of ATP-Binding Pocket.

Authors:  Hirofumi Nakano; Tsukasa Hasegawa; Hirotatsu Kojima; Takayoshi Okabe; Tetsuo Nagano
Journal:  ACS Med Chem Lett       Date:  2017-04-03       Impact factor: 4.345

2.  Characterization of HJ-PI01 as a novel Pim-2 inhibitor that induces apoptosis and autophagic cell death in triple-negative human breast cancer.

Authors:  Yu-Qian Zhao; Yi-Qiong Yin; Jie Liu; Gui-Hua Wang; Jian Huang; Ling-Juan Zhu; Jin-Hui Wang
Journal:  Acta Pharmacol Sin       Date:  2016-07-11       Impact factor: 6.150

3.  Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.

Authors:  Matthew T Burger; Wooseok Han; Jiong Lan; Gisele Nishiguchi; Cornelia Bellamacina; Mika Lindval; Gordana Atallah; Yu Ding; Michelle Mathur; Chris McBride; Elizabeth L Beans; Kristine Muller; Victoriano Tamez; Yanchen Zhang; Kay Huh; Paul Feucht; Tatiana Zavorotinskaya; Yumin Dai; Jocelyn Holash; Joseph Castillo; John Langowski; Yingyun Wang; Min Y Chen; Pablo D Garcia
Journal:  ACS Med Chem Lett       Date:  2013-10-15       Impact factor: 4.345

4.  Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.

Authors:  Theresa D Manz; Sindhu Carmen Sivakumaren; Fleur M Ferguson; Tinghu Zhang; Adam Yasgar; Hyuk-Soo Seo; Scott B Ficarro; Joseph D Card; Hyeseok Shim; Chandrasekhar V Miduturu; Anton Simeonov; Min Shen; Jarrod A Marto; Sirano Dhe-Paganon; Matthew D Hall; Lewis C Cantley; Nathanael S Gray
Journal:  J Med Chem       Date:  2020-04-27       Impact factor: 7.446

5.  AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia.

Authors:  Erika K Keeton; Kristen McEachern; Keith S Dillman; Sangeetha Palakurthi; Yichen Cao; Michael R Grondine; Surinder Kaur; Suping Wang; Yuching Chen; Allan Wu; Minhui Shen; Francis D Gibbons; Michelle L Lamb; Xiaolan Zheng; Richard M Stone; Daniel J Deangelo; Leonidas C Platanias; Les A Dakin; Huawei Chen; Paul D Lyne; Dennis Huszar
Journal:  Blood       Date:  2013-12-20       Impact factor: 22.113

6.  Discovery and identification of PIM-1 kinase inhibitors through a hybrid screening approach.

Authors:  Mingfeng Shao; Yiming Yuan; Kun Yu; Kai Lei; Guonian Zhu; Lijuan Chen; Mingli Xiang
Journal:  Mol Divers       Date:  2014-02-12       Impact factor: 2.943

7.  Pim2 is required for maintaining multiple myeloma cell growth through modulating TSC2 phosphorylation.

Authors:  Jing Lu; Tatiana Zavorotinskaya; Yumin Dai; Xiao-Hong Niu; Joseph Castillo; Janet Sim; Jianjun Yu; Yingyun Wang; John L Langowski; Jocelyn Holash; Kevin Shannon; Pablo D Garcia
Journal:  Blood       Date:  2013-07-01       Impact factor: 22.113

8.  STAT5 is essential for IL-7-mediated viability, growth, and proliferation of T-cell acute lymphoblastic leukemia cells.

Authors:  Daniel Ribeiro; Alice Melão; Ruben van Boxtel; Cristina I Santos; Ana Silva; Milene C Silva; Bruno A Cardoso; Paul J Coffer; João T Barata
Journal:  Blood Adv       Date:  2018-09-11

Review 9.  Pathophysiological roles of Pim-3 kinase in pancreatic cancer development and progression.

Authors:  Ying-Yi Li; Naofumi Mukaida
Journal:  World J Gastroenterol       Date:  2014-07-28       Impact factor: 5.742

10.  Synergistic PIM kinase and proteasome inhibition as a therapeutic strategy for MYC-overexpressing triple-negative breast cancer.

Authors:  Ratika Kunder; Michelle Velyunskiy; Sara F Dunne; Byoung-Kyu Cho; Deepak Kanojia; Lauren Begg; Adrienne M Orriols; Erica Fleming-Trujillo; Pranathi Vadlamani; Alesia Vialichka; Rosemary Bolin; Jessica N Perrino; Diane Roth; Matthew R Clutter; Nicolette A Zielinski-Mozny; Young Ah Goo; Massimo Cristofanilli; Marc L Mendillo; Athanassios Vassilopoulos; Dai Horiuchi
Journal:  Cell Chem Biol       Date:  2021-09-14       Impact factor: 8.116
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