Synthesis and Antileukemia Activity Evaluation of Benzophenanthridine Alkaloid Derivatives.

ABSTRACT: Thirty-three benzophenanthridine alkaloid derivatives (1a-1u and 2a-2l) were synthesized, and their cytotoxic activities against two leukemia cell lines (Jurkat Clone E6-1 and THP-1) were evaluated in vitro using a Cell Counting Kit-8 (CCK-8) assay. Nine of these derivatives (1i-l, 2a, and 2i-l) with IC₅₀ values in the range of 0.18-7.94 μM showed significant inhibitory effects on the proliferation of both cancer cell lines. Analysis of the primary structure-activity relationships revealed that different substituent groups at the C-6 position might have an effect on the antileukemia activity of the corresponding compounds. In addition, the groups at the C-7 and C-8 positions could influence the antileukemia activity.

SUBMITTER: Tang Y 

PROVIDER: S-EPMC9227418 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature