1366595-48-3Relevant academic research and scientific papers
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
, p. 4613 - 4619 (2016)
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.
4-Connected azabicyclo[5.3.0]decane Smac mimetics-Zn2+ chelators as dual action antitumoral agents
Manzoni, Leonardo,Samela, Alessandro,Barbini, Stefano,Cairati, Silvia,Penconi, Marta,Arosio, Daniela,Lecis, Daniele,Seneci, Pierfausto
supporting information, p. 2336 - 2344 (2017/05/10)
Putative dual action compounds (DACs 3a–d) based on azabicyclo[5.3.0]decane (ABD) Smac mimetic scaffolds linked to Zn2+-chelating 2,2′-dipicolylamine (DPA) through their 4 position are reported and characterized. Their synthesis, their target a
Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents
Bianchi, Aldo,Ugazzi, Marcello,Ferrante, Luca,Lecis, Daniele,Scavullo, Cinzia,Mastrangelo, Eloise,Seneci, Pierfausto
supporting information; experimental part, p. 2204 - 2208 (2012/04/18)
A set of phenyl-substituted Smac mimetics/IAP inhibitor analogues of lead compound 2a was synthesized, aiming to retain its strong cell-free potency while increasing its bioavailability. Seventeen compounds 2b-r were prepared and characterized in vitro, u
