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

Sabrina Taliani 1, * Isabella Pugliesi 1 Elisabetta Barresi 1 Silvia Salerno 1 Christophe Marchand 2 Keli Agama 2 Francesca Simorini 1 Concettina La Motta 1 Anna Maria Marini 1 Francesco Saverio Di Leva Luciana Marinelli Sandro Cosconati 3 Ettore Novellino 4 Yves Pommier 5 Roberto Di Santo 6 Federico da Settimo 1
* Corresponding author
1 Department of Pharmacy
2 Laboratory of Molecular Pharmacology
3 Department of Pharmaceutical Chemistry and Toxicology
4 Department of Pharmacy Naples
5 Laboratory of Molecular Pharmacology
6 Department of Medicinal Chemistry and Technologies
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.
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Sabrina Taliani, Isabella Pugliesi, Elisabetta Barresi, Silvia Salerno, Christophe Marchand, et al.. Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.. Journal of Medicinal Chemistry, American Chemical Society, 2013, 56 (18), pp.7458-62. ⟨10.1021/jm400932c⟩. ⟨pasteur-00968854⟩

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