In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted phenyl ring at 2- or 3-position, a protonable side chain at 4- or 5-position), affording a number of Top1 inhibitors with cleavage patterns common to CPT and MJ-III-65. SARs data were rationalized by means of an advanced docking protocol.

Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of non-camptothecin Topoisomerase I (Top1) inhibitors

TALIANI, SABRINA
Primo
;
BARRESI, ELISABETTA;SALERNO, SILVIA;SIMORINI, FRANCESCA;LA MOTTA, CONCETTINA;MARINI, ANNA MARIA;DA SETTIMO PASSETTI, FEDERICO
Ultimo
2013

Abstract

In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related to the indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., a substituted phenyl ring at 2- or 3-position, a protonable side chain at 4- or 5-position), affording a number of Top1 inhibitors with cleavage patterns common to CPT and MJ-III-65. SARs data were rationalized by means of an advanced docking protocol.
Taliani, Sabrina; Isabella, Pugliesi; Barresi, Elisabetta; Salerno, Silvia; Christophe, Marchand; Keli, Agama; Simorini, Francesca; LA MOTTA, Concettina; Marini, ANNA MARIA; Francesco Saverio Di, Leva; Luciana, Marinelli; Sandro, Cosconati; Ettore, Novellino; Yves, Pommier; Roberto Di, Santo; DA SETTIMO PASSETTI, Federico
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/260137
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