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Journal articles
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
Sabrina Taliani 1
Correspondent author
Isabella Pugliesi 1
Author
Elisabetta Barresi 1
Author
Silvia Salerno 1
Author
Christophe Marchand 2
Author
Keli Agama 2
Author
Francesca Simorini 1
Author
Concettina La Motta 1
Author
Anna Maria Marini 1
Author
Francesco Saverio Di Leva
Author
Luciana Marinelli
Author
Sandro Cosconati 3
Author
Ettore Novellino 4
Author
Yves Pommier 5
Author
Roberto Di Santo 6
Author
Federico da Settimo 1
Author
1
Department of Pharmacy (Italy)
- University of Pisa - Università di Pisa (Lungarno Pacinotti 43 - 56126 Pisa - Italy)
2
Laboratory of Molecular Pharmacology (Center for Cancer Research, Bethesda, Maryland 20892-4255 - United States)
- NCI-NIH - National Cancer Institute [Bethesda] (BG 9609 MSC 9760, 9609 Medical Center Drive, Bethesda, MD 20892-9760 - United States)
- NIH - National Institutes of Health [Bethesda] (9000 Rockville Pike, Bethesda, Maryland 20892 - United States)
3
Department of Pharmaceutical Chemistry and Toxicology (Italy)
- Università degli studi di Napoli Federico II (Corso Umberto I 40 - 80138 Napoli - Italy)
4
Department of Pharmacy Naples (University of Naples Federico II, via D. Montesano 49, I-80131 Naples - Italy)
- Université de Naples (France)
5
Laboratory of Molecular Pharmacology (National Cancer Institute Bldg. 37, Room 4E28 37 Convent Drive MSC 4255 Bethesda, MD 20892-4255 - France)
- NIH - National Institutes of Health [Bethesda] (9000 Rockville Pike, Bethesda, Maryland 20892 - United States)
- NCI-NIH - National Cancer Institute [Bethesda] (BG 9609 MSC 9760, 9609 Medical Center Drive, Bethesda, MD 20892-9760 - United States)
- NIH - National Institutes of Health [Bethesda] (9000 Rockville Pike, Bethesda, Maryland 20892 - United States)
6
Department of Medicinal Chemistry and Technologies (Piazzale Aldo Moro 5, I-00185, Rome - Italy)
- Institut Pasteur, Fondation Cenci Bolognetti - Istituto Pasteur Italia, Fondazione Cenci Bolognetti (Université de Rome La Sapienza 5 Place Aldo Moro 00185 Rome - Italy)
- RIIP - Réseau International des Instituts Pasteur (25, rue du Dr Roux 75724 Paris Cedex 15 - France)
- Università degli Studi di Roma "La Sapienza" [Rome] (Piazzale Aldo Moro 5, 00185 Roma - Italy)
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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https://hal-riip.archives-ouvertes.fr/pasteur-00968854
Contributor : Istituto Pasteur Fondazione Cenci Bolognetti <>
Submitted on : Tuesday, April 1, 2014 - 4:22:29 PM
Last modification on : Wednesday, October 28, 2020 - 3:20:08 PM
Long-term archiving on: : Monday, April 10, 2017 - 8:18:18 AM
Contributor : Istituto Pasteur Fondazione Cenci Bolognetti <>
Submitted on : Tuesday, April 1, 2014 - 4:22:29 PM
Last modification on : Wednesday, October 28, 2020 - 3:20:08 PM
Long-term archiving on: : Monday, April 10, 2017 - 8:18:18 AM
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Identifiers
- HAL Id : pasteur-00968854, version 1
- DOI : 10.1021/jm400932c
- PUBMED : 23987476
Citation
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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