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Discovery of a Potent Anticancer Agent PVHD303 with in Vivo Activity.

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.

SUBMITTER: Suzuki Y

PROVIDER: S-EPMC7294709 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature

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Discovery of a Potent Anticancer Agent PVHD303 with in Vivo Activity.

Suzuki Yumiko Y Otake Ayana A Ueno Satoshi S Hayashi Kensuke K Ishii Hirosuke H Miyoshi Nao N Kuroiwa Kenta K Tachikawa Masashi M Fujimaki Yuki Y Nishiyama Kotaro K Manabe Kei K Yamazaki Ryuta R Asai Akira A

ACS medicinal chemistry letters 20200508 6

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 th ...[more]

PMID: 32551013

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