Modified Benzoxazole-Based VEGFR-2 Inhibitors and Apoptosis Inducers: Design, Synthesis, and Anti-Proliferative Evaluation.

ABSTRACT: This work is one of our efforts to discover potent anticancer agents. We modified the most promising derivative of our previous work concerned with the development of VEGFR-2 inhibitor candidates. Thirteen new compounds based on benzoxazole moiety were synthesized and evaluated against three human cancer cell lines, namely, breast cancer (MCF-7), colorectal carcinoma (HCT116), and hepatocellular carcinoma (HepG2). The synthesized compounds were also evaluated against VEGFR-2 kinase activity. The biological testing fallouts showed that compound 8d was more potent than standard sorafenib. Such compound showed IC₅₀ values of 3.43, 2.79, and 2.43 µM against the aforementioned cancer cell lines, respectively, compared to IC₅₀ values of 4.21, 5.30, and 3.40 µM report

SUBMITTER: Elwan A 

PROVIDER: S-EPMC9370530 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature