Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein

Fedele Manna; Franco Chimenti; Rossella Fioravanti; Adriana Bolasco; Daniela Secci; Paola Chimenti; Cristiano Ferlini; Giovanni Scambia

doi:10.1016/j.bmcl.2005.05.067

Synthesis of some pyrazole derivatives and preliminary investigation of their affinity binding to P-glycoprotein

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4632-5. doi: 10.1016/j.bmcl.2005.05.067.

Authors

Fedele Manna¹, Franco Chimenti, Rossella Fioravanti, Adriana Bolasco, Daniela Secci, Paola Chimenti, Cristiano Ferlini, Giovanni Scambia

Affiliation

¹ Dip. di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy.

PMID: 16099651
DOI: 10.1016/j.bmcl.2005.05.067

Abstract

A series of substituted pyrazolines were synthesized and evaluated for their anticancer activity and for their ability to inhibit P-glycoprotein-mediated multidrug resistance by direct binding to a purified protein domain containing an ATP-binding site and a modulator interacting region. Compounds 2a and e have been found to bind to P-glycoprotein with greater affinity.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / metabolism
Magnetic Resonance Spectroscopy
Protein Binding
Pyrazoles / chemical synthesis*
Pyrazoles / metabolism
Spectrophotometry, Ultraviolet

Substances

ATP Binding Cassette Transporter, Subfamily B, Member 1
Antineoplastic Agents
Pyrazoles