One-pot synthesis, anti-tumor evaluation and structure-activity relationships of novel 25-OCH₃-PPD derivatives.

ABSTRACT: Based on the fact that 25-OCH₃-PPD, a natural ginsengenin isolated from the leaves of Panax ginseng, is a promising lead compound, novel 25-OCH₃-PPD derivatives were synthesized to find more potent anti-tumor agents by a simple and facile synthetic method. These derivatives were classified into three types and screened for their cytotoxic activities against seven human cancer cell lines. Compared with 25-OCH₃-PPD, compounds a5, a7, b5 and b7 exhibited higher anti-tumor activities on all tested cell lines with almost 5-fold to 15-fold increases. In particular, compound a7 showed the greatest cytotoxic activity against α-2 cells (IC₅₀ = 2.4 ± 0.4 μM). The preliminary study on the mechanisms indicated that c

SUBMITTER: Qu FZ 

PROVIDER: S-EPMC6084169 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature