A set of phenyl-substituted Smac mimetics/IAP inhibitor analogs of lead compd. I [R = H] was synthesized, aiming to retain its strong cell-free potency while increasing its bioavailability. Seventeen compds. were prepd. and characterized in vitro, using cell-free and cellular assays. Among them, I [R = CF3] showed the best permeability through cell membranes, and was selected for further in vitro and in vivo studies due to its strong, sub-micromolar cellular potency.

Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents / A. Bianchi, M. Ugazzi, L. Ferrante, D. Lecis, C. Scavullo, E. Mastrangelo, P. Seneci. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 22:6(2012), pp. 2204-2208. [10.1016/j.bmcl.2012.01.098]

Rational design, synthesis and characterization of potent, drug-like monomeric Smac mimetics as pro-apoptotic anticancer agents

P. Seneci
Ultimo
2012

Abstract

A set of phenyl-substituted Smac mimetics/IAP inhibitor analogs of lead compd. I [R = H] was synthesized, aiming to retain its strong cell-free potency while increasing its bioavailability. Seventeen compds. were prepd. and characterized in vitro, using cell-free and cellular assays. Among them, I [R = CF3] showed the best permeability through cell membranes, and was selected for further in vitro and in vivo studies due to its strong, sub-micromolar cellular potency.
Apoptosis; IAP inhibitors; Oncology; Peptidomimetics; Smac mimetics
Settore CHIM/06 - Chimica Organica
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/13 - Biologia Applicata
2012
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/191135
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