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New immunomodulatory anticancer quinazolinone-based thalidomide analogs: design, synthesis and biological evaluation.


ABSTRACT: Aim: The current work is an extension to our previous work for the development of new thalidomide analogs.Materials & methods: Quinazolinone-based molecules carrying a glutarimide moiety have been designed, synthesized and biologically evaluated for immunomodulatory and anticancer activity.Results: Compounds 7d and 12 showed considerable immunomodulatory properties in comparison to thalidomide. 7d and 12 significantly reduced TNF-α levels in HepG-2 cells from 162.5 to 57.4 pg/ml and 49.2 pg/ml, respectively, compared with 53.1 pg/ml reported for thalidomide. Moreover, they caused 69.33 and 77.74% reduction in NF-κB P65, respectively, compared with 60.26% reduction for thalidomide. Similarly, they reduced VEGF from 432.5 to 161.3 pg/ml and 13

SUBMITTER: Saleh Al Ward MM 

PROVIDER: S-EPMC11622738 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature