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)

Aiello, Stefania, Wells, Geoffrey, Stone, Erica L., Kadri, Hachemi, Bazzi, Rana, Bell, David R., Stevens, Malcolm F. G., Matthews, Charles S., Bradshaw, Tracey D. and Westwell, Andrew D. (2008) 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). Journal of Medicinal Chemistry, 51(16), pp. 5135-5139. ISSN (print) 0022-2623

Official URL: https://doi.org/10.1021/jm800418z

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.

Actions (Repository Editors)

Item Control Page