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)

被引：315

作者：

Aiello, Stefania ^{[1
,2
]}

Wells, Geoffrey ^{[3
]}

Stone, Erica L. ^{[4
]}

Kadri, Hachemi ^{[1
]}

Bazzi, Rana ^{[5
]}

Bell, David R. ^{[5
]}

Stevens, Malcolm F. G. ^{[3
,4
]}

Matthews, Charles S. ^{[4
]}

Bradshaw, Tracey D. ^{[4
]}

Westwell, Andrew D. ^{[1
]}

机构：

[1] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3NB, S Glam, Wales

[2] Univ Palermo, Fac Farm, Dipartimento Farmacochim Tossicolog & Biol, I-90123 Palermo, Italy

[3] Pharminox Ltd, Nottingham NG1 1GF, England

[4] Univ Nottingham, Sch Pharm, Ctr Biomol Sci, Nottingham NG7 2RD, England

[5] Univ Nottingham, Sch Biol, Nottingham NG7 2RD, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 16期

关键词：

D O I：

10.1021/jm800418z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 GI(50) 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.

引用

页码：5135 / 5139

页数：5

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