1099616-09-7Relevant articles and documents
Dual action Smac mimetics–zinc chelators as pro-apoptotic antitumoral agents
Manzoni, Leonardo,Gornati, Davide,Manzotti, Mattia,Cairati, Silvia,Bossi, Alberto,Arosio, Daniela,Lecis, Daniele,Seneci, Pierfausto
supporting information, p. 4613 - 4619 (2016/09/13)
Dual action compounds (DACs) based on 4-substituted aza-bicyclo[5.3.0]decane Smac mimetic scaffolds (ABDs) linked to a Zn2+-chelating moiety (DPA, o-hydroxy, m-allyl, N-acyl (E)-phenylhydrazone) through their 10 position are reported and characterized. Their synthesis, their target affinity (XIAP BIR3, Zn2+) in cell-free assays, their pro-apoptotic effects and cytotoxicity in tumor cells with varying sensitivity to Smac mimetics are described. The results are interpreted to evaluate the influence of Zn2+chelators on cell-free potency and on cellular permeability of DACs, and to propose novel avenues towards more potent antitumoral DACs based on Smac mimetics and Zn2+chelation.
NEW SMAC MIMETIC COMPOUNDS AS APOPTOSIS INDUCERS
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Page/Page column 40-41, (2009/06/27)
The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of a