%0 Journal Article %T Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors. %+ Department of Pharmacy %+ Laboratory of Molecular Pharmacology %+ Department of Pharmaceutical Chemistry and Toxicology %+ Department of Pharmacy Naples %+ Laboratory of Molecular Pharmacology %+ Department of Medicinal Chemistry and Technologies %A Taliani, Sabrina %A Pugliesi, Isabella %A Barresi, Elisabetta %A Salerno, Silvia %A Marchand, Christophe %A Agama, Keli %A Simorini, Francesca %A La Motta, Concettina %A Marini, Anna Maria %A Di Leva, Francesco Saverio %A Marinelli, Luciana %A Cosconati, Sandro %A Novellino, Ettore %A Pommier, Yves %A Di Santo, Roberto %A da Settimo, Federico %< avec comité de lecture %@ 0022-2623 %J Journal of Medicinal Chemistry %I American Chemical Society %V 56 %N 18 %P 7458-62 %8 2013-09-26 %D 2013 %R 10.1021/jm400932c %M 23987476 %Z Life Sciences [q-bio]/Pharmaceutical sciencesJournal articles %X 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. %G English %2 https://riip.hal.science/pasteur-00968854/document %2 https://riip.hal.science/pasteur-00968854/file/Talianietal2013.pdf %L pasteur-00968854 %U https://riip.hal.science/pasteur-00968854 %~ RIIP %~ RIIP_FCB