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Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents.

Abstract：

:Three series of novel 4-benzothiazole amino quinazolines Dasatinib derivatives have been designed and synthesized. The entire target compounds were investigated for their in vitro cytotoxic activity by the MTT-based assay against 6 human cancer cell lines. Compared with the parental Dasatinib, most of the new compounds, especially 2, 4, 6-trimethylaniline series (3), demonstrated significant inhibitory activities against six cell lines. Furthermore, the target compounds were screened for Src and Abl kinase inhibitory activity. Among them, 1a, 1f and 3a-3f are more potential dual Src/Abl kinase inhibitors. Thus they may be promising lead compounds to be developed as an alternative for current Dasatinib therapy or for Imatinib-resistant patients, potentially via simultaneously blocking multiple RTK signaling pathways.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Cai J,Sun M,Wu X,Chen J,Wang P,Zong X,Ji M

doi

10.1016/j.ejmech.2013.03.013

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

702-12

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00161-X

journal_volume

63

pub_type

杂志文章

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