Design, synthesis and biological activity evaluation of 2-mercapto-4(3H)-quinazolinone derivatives as novel inhibitors of protein tyrosine phosphatase 1B

Hui Li; Jin Ping Wang; Fan Yang; Ting Liu; Wen Wei Qiu; Jing Ya Li; Jia Li; Jie Tang

doi:10.3987/COM-12-12477

Design, synthesis and biological activity evaluation of 2-mercapto-4(3H)-quinazolinone derivatives as novel inhibitors of protein tyrosine phosphatase 1B

Hui Li
, Jin Ping Wang
, Fan Yang
, Ting Liu
, Wen Wei Qiu
, Jing Ya Li
, Jia Li
, Jie Tang^*

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

Research output: Contribution to journal › Article › peer-review

11 Scopus citations

Abstract

A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC ₅₀ = 1.50 μ ;g/mL), and 27 possessed the best selectivity of 3.0-fold.

Original language	English
Pages (from-to)	1897-1911
Number of pages	15
Journal	Heterocycles
Volume	85
Issue number	8
DOIs	https://doi.org/10.3987/COM-12-12477
State	Published - 2012

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title = "Design, synthesis and biological activity evaluation of 2-mercapto-4(3H)-quinazolinone derivatives as novel inhibitors of protein tyrosine phosphatase 1B",

abstract = "A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC 50 = 1.50 μ ;g/mL), and 27 possessed the best selectivity of 3.0-fold.",

author = "Hui Li and Wang, \{Jin Ping\} and Fan Yang and Ting Liu and Qiu, \{Wen Wei\} and Li, \{Jing Ya\} and Jia Li and Jie Tang",

year = "2012",

doi = "10.3987/COM-12-12477",

language = "英语",

volume = "85",

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journal = "Heterocycles",

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publisher = "Japan Institute of Heterocyclic Chemistry",

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T1 - Design, synthesis and biological activity evaluation of 2-mercapto-4(3H)-quinazolinone derivatives as novel inhibitors of protein tyrosine phosphatase 1B

AU - Li, Hui

AU - Wang, Jin Ping

AU - Yang, Fan

AU - Liu, Ting

AU - Qiu, Wen Wei

AU - Li, Jing Ya

AU - Li, Jia

AU - Tang, Jie

PY - 2012

Y1 - 2012

N2 - A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC 50 = 1.50 μ ;g/mL), and 27 possessed the best selectivity of 3.0-fold.

AB - A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC 50 = 1.50 μ ;g/mL), and 27 possessed the best selectivity of 3.0-fold.

UR - https://www.scopus.com/pages/publications/84864359321

U2 - 10.3987/COM-12-12477

DO - 10.3987/COM-12-12477

M3 - 文章

AN - SCOPUS:84864359321

SN - 0385-5414

VL - 85

SP - 1897

EP - 1911

JO - Heterocycles

JF - Heterocycles

IS - 8

ER -

Design, synthesis and biological activity evaluation of 2-mercapto-4(3H)-quinazolinone derivatives as novel inhibitors of protein tyrosine phosphatase 1B

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