Literature DB >> 18951019

2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase).

Joseph S Warmus1, Cathlin Flamme, Lu Yan Zhang, Stephen Barrett, Alexander Bridges, Huifen Chen, Richard Gowan, Michael Kaufman, Judy Sebolt-Leopold, Wilbur Leopold, Ronald Merriman, Jeffrey Ohren, Alexander Pavlovsky, Sally Przybranowski, Haile Tecle, Heather Valik, Christopher Whitehead, Erli Zhang.   

Abstract

This paper reports a second generation MEK inhibitor. The previously reported potent and efficacious MEK inhibitor, PD-184352 (CI-1040), contains an integral hydroxamate moiety. This compound suffered from less than ideal solubility and metabolic stability. An oxadiazole moiety behaves as a bioisostere for the hydroxamate group, leading to a more metabolically stable and efficacious MEK inhibitor.

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Year:  2008        PMID： 18951019     DOI： 10.1016/j.bmcl.2008.10.015

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


  9 in total

1.  Synthesis and evaluation of sulfonylnitrophenylthiazoles (SNPTs) as thyroid hormone receptor-coactivator interaction inhibitors.

Authors:  Jong Yeon Hwang; Ramy R Attia; Fangyi Zhu; Lei Yang; Andrew Lemoff; Cynthia Jeffries; Michele C Connelly; R Kiplin Guy
Journal:  J Med Chem       Date:  2012-02-23       Impact factor: 7.446

2.  Development of a novel thymidylate synthase (TS) inhibitor capable of up-regulating P53 expression and inhibiting angiogenesis in NSCLC.

Authors:  Xin-Yang Li; De-Pu Wang; Guo-Qing Lu; Kai-Li Liu; Ting-Jian Zhang; Shuai Li; Kamara Mohamed O; Wen-Han Xue; Xin-Hua Qian; Fan-Hao Meng
Journal:  J Adv Res       Date:  2020-07-25       Impact factor: 10.479

3.  Structural Requirements and Docking Analysis of Amidine-Based Sphingosine Kinase 1 Inhibitors Containing Oxadiazoles.

Authors:  Joseph D Houck; Thomas K Dawson; Andrew J Kennedy; Yugesh Kharel; Niels D Naimon; Saundra D Field; Kevin R Lynch; Timothy L Macdonald
Journal:  ACS Med Chem Lett       Date:  2016-03-01       Impact factor: 4.345

4.  Specific Noncovalent Interactions Determine Optimal Structure of a Buried Ligand Moiety: QM/MM and Pure QM Modeling of Complexes of the Small-Molecule CD4 Mimetics and HIV-1 gp120.

Authors:  Francesca Moraca; David Rinaldo; Amos B Smith; Cameron F Abrams
Journal:  ChemMedChem       Date:  2018-02-09       Impact factor: 3.466

5.  Cofactor-mediated conformational control in the bifunctional kinase/RNase Ire1.

Authors:  Alexei V Korennykh; Pascal F Egea; Andrei A Korostelev; Janet Finer-Moore; Robert M Stroud; Chao Zhang; Kevan M Shokat; Peter Walter
Journal:  BMC Biol       Date:  2011-07-06       Impact factor: 7.431

Review 6.  Role and mechanism of action of leucine-rich repeat kinase 1 in bone.

Authors:  Weirong R Xing; Helen Goodluck; Canjun Zeng; Subburaman Mohan
Journal:  Bone Res       Date:  2017-03-14       Impact factor: 13.567

7.  A small molecular inhibitor of LRRK1 identified by homology modeling and virtual screening suppresses osteoclast function, but not osteoclast differentiation, in vitro.

Authors:  Mingjue Si; Canjun Zeng; Helen Goodluck; Sandi Shen; Subburaman Mohan; Weirong Xing
Journal:  Aging (Albany NY)       Date:  2019-05-21       Impact factor: 5.682

8.  Polypharmacology of Berberine Based on Multi-Target Binding Motifs.

Authors:  Ming Chu; Xi Chen; Jing Wang; Likai Guo; Qianqian Wang; Zirui Gao; Jiarui Kang; Mingbo Zhang; Jinqiu Feng; Qi Guo; Binghua Li; Chengrui Zhang; Xueyuan Guo; Zhengyun Chu; Yuedan Wang
Journal:  Front Pharmacol       Date:  2018-07-24       Impact factor: 5.810

9.  UV-Induced 1,3,4-Oxadiazole Formation from 5-Substituted Tetrazoles and Carboxylic Acids in Flow.

Authors:  Luke Green; Keith Livingstone; Sophie Bertrand; Simon Peace; Craig Jamieson
Journal:  Chemistry       Date:  2020-10-12       Impact factor: 5.236
  9 in total

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