Succinamide derivatives of melampomagnolide B and their anti-cancer activities.

ABSTRACT: A series of succinamide derivatives of melampomagnolide B have been synthesized by coupling MMB monosuccinate (2) with various heterocyclic amines to afford compounds 3a-3l. MMB monosuccinate was also reacted with terminal diaminoalkanes to afford dimeric succinamido analogs of MMB (4a-4h). These succinamide analogs of MMB were evaluated for their anti-cancer activity against a panel of sixty human cancer cell lines. Analogs 3d-3i and dimers 4f-4g exhibited promising anti-cancer activity with GI₅₀ values ranging from 0.28 to 33.5µM against most of the cell lines in the panel. The dimeric analogs 4f and 4g were identified as lead compounds with GI₅₀ values in the nanomolar range (GI₅₀=280-980nM) against several cell lines in the panel; i.e. leukemia cell lin

SUBMITTER: Janganati V 

PROVIDER: S-EPMC5531864 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature