Design, synthesis, and biological evaluation of novel bioactive thalidomide analogs as anticancer immunomodulatory agents† † Electronic supplementary information (ESI) available. See DOI: https://doi.org/10.1039/d2ra06188k

ABSTRACT: Cancer is still a dangerous disease with a high mortality rate all over the world. In our attempt to develop potential anticancer candidates, new quinazoline and phthalazine based compounds were designed and synthesized. The new derivatives were built in line with the pharmacophoric features of thalidomide. The new derivatives as well as thalidomide were examined against three cancer cell lines, namely: hepatocellular carcinoma (HepG-2), breast cancer (MCF-7) and prostate cancer (PC3). Then the effects on the expression levels of caspase-8, VEGF, NF-κB P65, and TNF-α in HepG-2 cells were evaluated. The biological data revealed the high importance of phthalazine based compounds (24a–c), which were far better than thalidomide with regard to the antiproliferative activity. 24b showed IC50 of

SUBMITTER: Kotb A 

PROVIDER: S-EPMC9680624 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature