Discovery of a Potent Anticancer Agent PVHD303 with in Vivo Activity

ACS Med Chem Lett. 2020 May 8;11(6):1287-1291. doi: 10.1021/acsmedchemlett.0c00119.

Yumiko Suzuki ¹, Ayana Otake ², Satoshi Ueno ³, Kensuke Hayashi ¹, Hirosuke Ishii ⁴, Nao Miyoshi ⁴, Kenta Kuroiwa ¹, Masashi Tachikawa ¹, Yuki Fujimaki ¹, Kotaro Nishiyama ¹, Kei Manabe ², Ryuta Yamazaki ³, Akira Asai ⁴

Affiliations

1 Department of Materials and Life Sciences, Faculty of Science and Technology, Sophia University, 7-1 Kioi-cho, Chiyoda-ku, Tokyo 102-8554, Japan.
2 School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
3 Pharmaceutical Research Department, Yakult Central Institute, 5-11 Izumi, Kunitachi-shi, Tokyo 186-8650, Japan.
4 Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.

PMID: 32551013 DOI: 10.1021/acsmedchemlett.0c00119

Abstract

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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