Synthesis and biological evaluation of N(9)-substituted harmine derivatives as potential anticancer agents.
Basic Information
ID: ALA4425146
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological evaluation of N(9)-substituted harmine derivatives as potential anticancer agents.
Authors: Du H, Tian S, Chen J, Gu H, Li N, Wang J.
Abstract: A series of N(9)-substituted harmine derivatives were synthesized and evaluated for their anticancer activity on a panel of cancer cell lines, their apoptosis induction and their cell cycle effects. The results showed that N(9)-substituted harmine derivatives had anticancer effects. In particular, N(9)-haloalkyl derivatives 9a-9c and N(9)-acyl harmine derivatives 11c and 11d, with IC50 values less than 1μM, were more potent than doxorubicin against A-549 and/or MCF-7 cell lines. Moreover, structure-activity relationships (SARs) indicated that introducing a haloalkyl or benzenesulfonyl group in the N(9)-position of harmine could significantly increase the anticancer activity. The most active compound (11d) caused cell cycle arrest in the G2/M phase, and induced cell apoptosis in a dose-dependent manner.
CiteXplore: 27397495
DOI: 10.1016/j.bmcl.2016.06.087
Patent ID: ┄