OPEN Foundation

Synthesis and biological evaluation of N(9)-substituted harmine derivatives as potential anticancer agents

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.
Du, H., Tian, S., Chen, J., Gu, H., Li, N., & Wang, J. (2016). Synthesis and biological evaluation of N 9-substituted harmine derivatives as potential anticancer agents. Bioorganic & medicinal chemistry letters26(16), 4015-4019. 10.1016/j.bmcl.2016.06.087
Link to full text

OPEN Foundation

Share This Post

get the latest

The OPEN Minded Newsletter keeps you informed about the latest psychedelic research & news, articles, exclusive events, job opportunities, programmes, and free resources!

By clicking SUBSCRIBE, I confirm to receive emails from the OPEN Foundation and agree with its privacy policy.

interested in becoming a trained psychedelic-assisted therapist?

Management of Psychedelic-Related Complications - Online Event - Nov 20th