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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / pharmacology
-
Benzopyrans / chemical synthesis*
-
Benzopyrans / pharmacology
-
Benzothiazoles / chemical synthesis*
-
Benzothiazoles / pharmacology
-
Benzoxazoles / chemical synthesis*
-
Benzoxazoles / pharmacology
-
Breast Neoplasms / drug therapy
-
Cell Cycle / drug effects
-
Cell Line, Tumor
-
Humans
-
Receptors, Aryl Hydrocarbon / metabolism
-
Structure-Activity Relationship
Substances
-
2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole
-
Antineoplastic Agents
-
Benzopyrans
-
Benzothiazoles
-
Benzoxazoles
-
Receptors, Aryl Hydrocarbon