Biological Evaluation, Molecular Docking Analyses, and ADME Profiling of Certain New Quinazolinones as Anti-colorectal Agents.

ABSTRACT: Colorectal carcinogenesis is a complex process, which is linked to dysregulation of human secretory phospholipases A₂ (hsPLA₂-G-IIA, hsPLA₂-G-V, and hsPLA₂-G-X), proteases (cathepsin-B, collagenase, thrombin, elastase, and trypsin), carbohydrate hydrolyzing enzymes (α-amylase and α-glucosidase), and free radical generating enzyme (xanthine oxidoreductase (XOR)). Therefore, some new quinazolinones were synthesized and evaluated as inhibitors against this array of enzymes as well as cytotoxic agents on LoVo and HCT-116 cells of colorectal cancer. Compounds 3g, 10, 8, 3c, and 1c exhibited promising cytotoxic effects with IC₅₀ values ranging from 206.07 to 459.79 μM. Nine compounds showed pr

SUBMITTER: El-Sayed NNE 

PROVIDER: S-EPMC9178606 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature