6533b824fe1ef96bd12804f3
RESEARCH PRODUCT
Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole
Stefania AielloG WellsEl StoneH KadriR BazziDr BellMf StevensCs MatthewsTd BradshawAd Westwellsubject
Settore CHIM/08 - Chimica Farmaceuticafluorobenzothiazole antitumor agentdescription
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.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2008-01-01 |