Literature DB >> 21504850

Synthesis and biological evaluation of novel quinazoline-derived human Pin1 inhibitors.

Lina Zhu1, Jing Jin, Chang Liu, Chongjing Zhang, Yan Sun, Yanshen Guo, Decai Fu, Xiaoguang Chen, Bailing Xu.   

Abstract

A series of novel 2,4-disubstituted quinazoline derivatives were prepared and their inhibitory activities on hPin1 were evaluated. Of all the synthesized compounds, eight compounds displayed inhibitory activities with IC(50) value at the level of 10(-6)mol/L. Preliminary structure-activity relationships were analyzed in details and the binding mode of the titled compounds was predicted using FlexX algorithm. The design and optimization of novel small molecule Pin1 inhibitors will be guided by the results of this report.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21504850     DOI: 10.1016/j.bmc.2011.03.058

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

Review 1.  Chemical characteristics, synthetic methods, and biological potential of quinazoline and quinazolinone derivatives.

Authors:  Mohammad Asif
Journal:  Int J Med Chem       Date:  2014-11-12

2.  Synthesis of chalcone incorporated quinazoline derivatives as anticancer agents.

Authors:  Sapavat Madhavi; Reddymasu Sreenivasulu; Jyothsna Pragathi Yazala; Rudraraju Ramesh Raju
Journal:  Saudi Pharm J       Date:  2016-06-24       Impact factor: 4.330

3.  Phosphate-sensing with (di-(2-picolyl)amino)quinazolines based on a fluorescence on-off system.

Authors:  Kazusa Aoki; Ryuji Osako; Jiahui Deng; Takashi Hayashita; Takeshi Hashimoto; Yumiko Suzuki
Journal:  RSC Adv       Date:  2020-04-17       Impact factor: 3.361

  3 in total

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