Literature DB >> 24486134

Substituted piperidines as HDM2 inhibitors.

Yao Ma1, Brian R Lahue2, Gerald W Shipps2, Jeseca Brookes2, Yaolin Wang2.   

Abstract

Novel small molecule HDM2 inhibitor, substituted piperidine, was identified. Initial SAR study indicated potential for several position optimizations. Additional potency enhancement was achieved by introducing a sidechain off the aromatic ring. DMPK study of one of the active compounds has shown a moderate oral PK and reasonable bioavailability.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Cancer; HDM2; MDM2; Oncology; Small molecule inhibitor; Substituted piperidine; p53

Mesh：

Substances：

Year:  2014        PMID： 24486134     DOI： 10.1016/j.bmcl.2014.01.026

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


  4 in total

1.  Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.

Authors:  Yao Ma; Brian R Lahue; Craig R Gibeau; Gerald W Shipps; Stéphane L Bogen; Yaolin Wang; Zhuyan Guo; Timothy J Guzi
Journal:  ACS Med Chem Lett       Date:  2014-02-24       Impact factor: 4.345

2.  Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.

Authors:  Stéphane L Bogen; Weidong Pan; Craig R Gibeau; Brian R Lahue; Yao Ma; Latha G Nair; Elise Seigel; Gerald W Shipps; Yuan Tian; Yaolin Wang; Yinghui Lin; Ming Liu; Suxing Liu; Asra Mirza; Xiaoying Wang; Philip Lipari; Cynthia Seidel-Dugan; Daniel J Hicklin; W Robert Bishop; Diane Rindgen; Amin Nomeir; Winifred Prosise; Paul Reichert; Giovanna Scapin; Corey Strickland; Ronald J Doll
Journal:  ACS Med Chem Lett       Date:  2016-01-20       Impact factor: 4.345

Review 3.  Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.

Authors:  Yujun Zhao; Angelo Aguilar; Denzil Bernard; Shaomeng Wang
Journal:  J Med Chem       Date:  2014-11-14       Impact factor: 7.446

Review 4.  Chemical Variations on the p53 Reactivation Theme.

Authors:  Carlos J A Ribeiro; Cecília M P Rodrigues; Rui Moreira; Maria M M Santos
Journal:  Pharmaceuticals (Basel)       Date:  2016-05-13
  4 in total

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