Discovery of a Potent Anticancer Agent PVHD303 with in Vivo Activity

ACS Medicinal Chemistry Letters
2020.0

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 <i>in vivo</i>.

Knowledge Graph

Similar Paper

Discovery of a Potent Anticancer Agent PVHD303 with in Vivo Activity
ACS Medicinal Chemistry Letters 2020.0
Synthesis and Structure–Activity Relationship Study of 1-Phenyl-1-(quinazolin-4-yl)ethanols as Anticancer Agents
ACS Medicinal Chemistry Letters 2015.0
Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position
Bioorganic &amp; Medicinal Chemistry Letters 2016.0
6-Alkylamino- and 2,3-Dihydro-3‘-methoxy-2-phenyl-4-quinazolinones and Related Compounds:  Their Synthesis, Cytotoxicity, and Inhibition of Tubulin Polymerization
Journal of Medicinal Chemistry 2000.0
3-Substituted 7-Phenyl-Pyrroloquinolinones Show Potent Cytotoxic Activity in Human Cancer Cell Lines
Journal of Medicinal Chemistry 2007.0
Synthesis and in vitro antiproliferative evaluation of pyrimido[5,4-c]quinoline-4-(3H)-one derivatives
European Journal of Medicinal Chemistry 2012.0
Discovery of Novel Quinoline–Chalcone Derivatives as Potent Antitumor Agents with Microtubule Polymerization Inhibitory Activity
Journal of Medicinal Chemistry 2019.0
Synthesis of 8-Hydroxyquinoline Derivatives as Novel Antitumor Agents
ACS Medicinal Chemistry Letters 2013.0
2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: A novel class of antitumor agents
European Journal of Medicinal Chemistry 2009.0
Antitumor Agents. Part 204: Synthesis and Biological Evaluation of Substituted 2-Aryl Quinazolinones
Bioorganic &amp; Medicinal Chemistry Letters 2001.0