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.