Site-Selective Synthesis of C-17 Ester Derivatives of Natural Andrographolide for Evaluation as a Potential Anticancer Agent.

ABSTRACT: A library of 57 compounds of natural andrographolide was designed, synthesized, and screened for in vitro studies against four human cancer cell lines: A594, PC-3, MCF-7, and HCT-116. Most of the synthesized compounds displayed better cytotoxic profile against all tested cells compared to the parent andrographolide (1). The tested semisynthetic derivatives of andrographolide were found to be more sensitive toward lung carcinoma (A594) and prostate carcinoma (PC-3) cell lines. Among the synthesized compounds, the C-17 p-methoxy phenyl ester analog 8s inhibited cell proliferation effectively in A549 (IC₅₀: 6.6 μM) and PC-3 (IC₅₀: 5.9 μM) cell variants, and compound 9s exhibited the most potent activity against the A594 cell line, with

SUBMITTER: Kumar G 

PROVIDER: S-EPMC9933479 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature