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Discovery of 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate as a potential antiproliferative agent by inhibiting histone deacetylase.

Abstract：

:Twenty-one benzotriazoles (3-16 and 18-24) were synthesized and half of them (5, 8-16, 20, and 21) were reported for the first time. Their antiproliferative activities against three human cancer cells were assayed. It revealed that 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate (9) showed considerable activity against three human cancer cell lines with the half maximal inhibitory concentration (IC(50)) values of 1.2-2.4 nM, which were close to the value of the positive control, doxorubicin. Further investigation indicated compound 9 was a potential histone deacetylase inhibitor (IC(50)=9.4 μM) and its binding mode was simulated using docking method.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Fu J,Yang Y,Zhang XW,Mao WJ,Zhang ZM,Zhu HL

doi

10.1016/j.bmc.2010.10.049

subject

Has Abstract

pub_date

2010-12-15 00:00:00

pages

8457-62

issue

24

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00972-7

journal_volume

18

pub_type

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