Design, synthesis, and biological evaluation of new arjunolic acid derivatives as anticancer agents.

ABSTRACT: Arjunolic acid (AA) is a pentacyclic triterpenoid with promising anticancer properties. A series of novel AA derivatives containing a pentameric A-ring with an enal moiety, combined with additional modifications at C-28, were designed and prepared. The biological activity on the viability of human cancer and non-tumor cell lines was evaluated in order to identify the most promising derivatives. Additionally, a preliminary study of the structure-activity relationship was carried out. The most active derivative, derivative 26, also showed the best selectivity between malignant cells and non-malignant fibroblasts. For compound 26, the anticancer molecular mechanism of action in PANC-1 cells was further studied and the results showed that this derivative induced a cell-cycle arrest at G0/G1 ph

SUBMITTER: Goncalves BMF 

PROVIDER: S-EPMC9945870 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature