MMB triazole analogs are potent NF-κB inhibitors and anti-cancer agents against both hematological and solid tumor cells.

ABSTRACT: Triazole derivatives of melampomagnolide B (MMB) have been synthesized via click chemistry methodologies and screened against a panel of 60 human cancer cell lines. Several derivatives showed promising anti-cancer activity, affording growth inhibition (GI₅₀) values in the nanomolar range (GI₅₀ = 0.02-0.99 μM). Lead compound 7h exhibited EC₅₀ values of 400 nM and 700 nM, respectively, against two AML clinical specimens. Compound 7h was significantly more potent than parthenolide as an inhibitor of p65 phosphorylation in both hematological and solid tumor cell lines, indicating its ability to inhibit the NF-κB pathway. In TMD-231 breast cancer cells, treatment with 7h reduced DNA binding activity of NF-κB through inhibition of IKK-β mediated p65 phosphorylati

SUBMITTER: Janganati V 

PROVIDER: S-EPMC6281399 | biostudies-literature | 2018 Sep

REPOSITORIES: biostudies-literature