Anticancer activity of pyrimidodiazepines based on 2-chloro-4-anilinoquinazoline: synthesis, DNA binding and molecular docking.

ABSTRACT: Multidrug resistance to chemotherapy is a critical health problem associated with mutation of the therapeutic target. Therefore, the development of anticancer agents remains a challenge to overcome cancer cell resistance. Herein, a new series of quinazoline-based pyrimidodiazepines 16a-g were synthesized by the cyclocondensation reaction of 2-chloro-4-anilinoquinazoline-chalcones 14a-g with 2,4,5,6-tetraaminopyrimidine. All quinazoline derivatives 14a-g and 16a-g were selected by the U.S. National Cancer Institute (NCI) for testing their anticancer activity against 60 cancer cell lines of different panels of human tumors. Among the tested compounds, quinazoline-chalcone 14g displayed high antiproliferative activity with GI₅₀ values between 0.622-1.81 μM against K-562 (leukemia),

SUBMITTER: Cuartas V 

PROVIDER: S-EPMC9036565 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature