Discovery of a Potent Anticancer Agent PVHD303 with <i>in Vivo</i> Activity.
Suzuki Y, Otake A, Ueno S, Hayashi K, Ishii H, Miyoshi N, Kuroiwa K, Tachikawa M, Fujimaki Y, Nishiyama K, Manabe K, Yamazaki R, Asai A.
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 <i>in vivo</i>.