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.

AIELLO, S., WELLS, G., STONE, E.L., KADRI, H., BAZZI, R., BELL, D.R., et al. (2008). Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole. JOURNAL OF MEDICINAL CHEMISTRY, 51(16), 5135-5139 [10.1021/jm800418z].

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

AIELLO, Stefania;
2008

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.
Settore CHIM/08 - Chimica Farmaceutica
AIELLO, S., WELLS, G., STONE, E.L., KADRI, H., BAZZI, R., BELL, D.R., et al. (2008). Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole. JOURNAL OF MEDICINAL CHEMISTRY, 51(16), 5135-5139 [10.1021/jm800418z].
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10447/45625
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