Literature DB >> 18929486

Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.

Pei-Pei Kung1, Lee Funk, Jerry Meng, Michael Collins, Joe Zhongxiang Zhou, M Catherine Johnson, Anne Ekker, Jeff Wang, Pramod Mehta, Min-Jean Yin, Caroline Rodgers, Jay F Davies, Eileen Bayman, Tod Smeal, Karen A Maegley, Michael R Gehring.   

Abstract

Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay. A class of novel and potent small molecule Hsp90 inhibitors were thereby identified. Enantio-pure compounds 31 and 33 were potent in PGA-based competitive binding assay and inhibited proliferation of various human cancer cell lines in vitro, with IC(50) values averaging 20 nM.

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Year:  2008        PMID： 18929486     DOI： 10.1016/j.bmcl.2008.09.081

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


  6 in total

1.  Advances in the discovery and development of heat-shock protein 90 inhibitors for cancer treatment.

Authors:  Hardik J Patel; Shanu Modi; Gabriela Chiosis; Tony Taldone
Journal:  Expert Opin Drug Discov       Date:  2011-05       Impact factor: 6.098

2.  Design and Synthesis of Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors.

Authors:  David S Huang; Emmanuelle V LeBlanc; Tanvi Shekhar-Guturja; Nicole Robbins; Damian J Krysan; Juan Pizarro; Luke Whitesell; Leah E Cowen; Lauren E Brown
Journal:  J Med Chem       Date:  2019-09-26       Impact factor: 7.446

3.  Structural determination of three different series of compounds as Hsp90 inhibitors using 3D-QSAR modeling, molecular docking and molecular dynamics methods.

Authors:  Jianling Liu; Fangfang Wang; Zhi Ma; Xia Wang; Yonghua Wang
Journal:  Int J Mol Sci       Date:  2011-01-30       Impact factor: 5.923

Review 4.  Proposal of Dual Inhibitor Targeting ATPase Domains of Topoisomerase II and Heat Shock Protein 90.

Authors:  Kyu-Yeon Jun; Youngjoo Kwon
Journal:  Biomol Ther (Seoul)       Date:  2016-09-01       Impact factor: 4.634

5.  Dynamics revelation of conformational changes and binding modes of heat shock protein 90 induced by inhibitor associations.

Authors:  Jianzhong Chen; Jinan Wang; Fengbo Lai; Wei Wang; Laixue Pang; Weiliang Zhu
Journal:  RSC Adv       Date:  2018-07-16       Impact factor: 4.036

6.  In Vitro and In Vivo Evaluation of Polyherbal Formulation against Russell's Viper and Cobra Venom and Screening of Bioactive Components by Docking Studies.

Authors:  G Sakthivel; Amitabha Dey; Kh Nongalleima; Murthy Chavali; R S Rimal Isaac; N Surjit Singh; Lokesh Deb
Journal:  Evid Based Complement Alternat Med       Date:  2013-02-28       Impact factor: 2.629
  6 in total

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