TY - JOUR
T1 - Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole
AU - Aiello, Stefania
AU - Bazzi, Rana
AU - Kadri, Hachemi
AU - Westwell, Andrew D.
AU - Stone, Erica L.
AU - Aiello, Stefania
AU - Bradshaw, Tracey D.
AU - Matthews, Charles S.
AU - Wells, Geoffrey
AU - Stevens, Malcolm F. G.
AU - Bell, David R.
PY - 2008
Y1 - 2008
N2 - 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.
AB - 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.
UR - http://hdl.handle.net/10447/45625
M3 - Article
VL - 51
SP - 5135
EP - 5139
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
ER -