Synthesis and Antitumor Activity of 6-(2-Aminobenzo[]thiazol-5-yl) Quinazolin-4(3)-one Derivatives

Overview

Journal ACS Omega

Publisher American Chemical Society

Specialty Chemistry

Date 2025 Feb 24

PMID 39989817

Authors

Ailing Linghu

Lei Tang

Qing Li

Ting Zhong

Fang Luo

Xinran Zhao

Feng Zhang

Mingzhi Su

Yanhua Fan

Linzhen Li

Affiliations

Soon will be listed here.

Abstract

Quinazolinones are key scaffolds in anticancer drug development. We previously identified the lead compound from a series of 6-(1-benzo[]imidazol-6-yl) quinazolin-4(3)-one derivatives. In this study, we optimized to develop new 6-(2-aminobenzo[]thiazol-5-yl) quinazolin-4(3)-one derivatives, with compound showing the best antiproliferative activity against A549 lung cancer cells (IC: 0.44 μM) and good selectivity. Mechanistic studies revealed that compound induced G1-phase arrest, inhibited ALK/PI3K/AKT signaling, disrupted mitochondrial membrane potential, and promoted apoptosis. It also significantly inhibited spheroid formation in a 3D cell culture model. In summary, the results suggest that compound might have potential for the development of anticancer drugs.

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