As
a part of our continuous structure–activity relationship
(SAR) studies on 1-(quinazolin-4-yl)-1-(4-methoxyphenyl)ethan-1-ols,
the synthesis of derivatives and their cytotoxicity against the human
lung cancer cell line A549 were explored. This led to the discovery
of 1-(2-(furan-3-yl)quinazolin-4-yl)-1-(4-methoxyphenyl)ethan-1-ol
(PVHD303) with potent antiproliferative activity. PVHD303 disturbed
microtubule formation at the centrosomes and inhibited the growth
of tumors dose-dependently in the HCT116 human colon cancer xenograft
model in vivo.
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