当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648).

Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648).

Abstract：

:New fluorinated 2-aryl-benzothiazoles, -benzoxazoles, and -chromen-4-ones have been synthesized and their activity against MCF-7 and MDA 468 breast cancer cell lines compared with the potent antitumor benzothiazole 5. Analogues such as 9a, b and 12a, d yielded submicromolar GI50 values in both cell lines; however, none of the new compounds approached 5 in terms of antitumor potency. For 5, binding to the aryl hydrocarbon receptor appeared to be necessary but not sufficient for growth inhibition.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Aiello S,Wells G,Stone EL,Kadri H,Bazzi R,Bell DR,Stevens MF,Matthews CS,Bradshaw TD,Westwell AD

doi

10.1021/jm800418z

subject

Has Abstract

pub_date

2008-08-28 00:00:00

pages

5135-9

issue

16

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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