Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors.
作者： Sabrina Taliani , Isabella Pugliesi , Elisabetta Barresi , Silvia Salerno , Christophe Marchand
DOI: 10.1021/JM400932C
关键词:
摘要: In search for a novel chemotype to develop topoisomerase I (Top1) inhibitors, the pyrazolo[1,5-a]quinazoline nucleus, structurally related indenoisoquinoline system precursor of well-known Top1 poisons, was variously decorated (i.e., substituted phenyl ring at 2- or 3-position, protonable side chain 4- 5-position), affording number inhibitors with cleavage patterns common CPT and MJ-III-65. SARs data were rationalized by means an advanced docking protocol.
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