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Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2013 Sep 26; Vol. 56 (18), pp. 7458-62. Date of Electronic Publication: 2013 Sep 16. - Publication Year :
- 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.
- Subjects :
- DNA Topoisomerases, Type I chemistry
Heterocyclic Compounds, 3-Ring chemistry
Heterocyclic Compounds, 3-Ring metabolism
Humans
Molecular Docking Simulation
Protein Conformation
Pyrroles metabolism
Quinazolines metabolism
Topoisomerase I Inhibitors metabolism
DNA Topoisomerases, Type I metabolism
Drug Discovery
Heterocyclic Compounds, 3-Ring pharmacology
Pyrroles chemistry
Pyrroles pharmacology
Quinazolines chemistry
Quinazolines pharmacology
Topoisomerase I Inhibitors chemistry
Topoisomerase I Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1520-4804
- Volume :
- 56
- Issue :
- 18
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23987476
- Full Text :
- https://doi.org/10.1021/jm400932c