Abstract：
:Two series of indenoisoquinoline topoisomerase I inhibitors have been prepared to investigate optimal substituents on the indenone ring at the 9-position. The more exhaustive series was prepared using a nitrated isoquinoline ring that has been previously demonstrated to enhance biological activity. After preliminary biological evaluation, a more focused series of inhibitors was prepared utilizing a 2,3-dimethoxy-substituted isoquinoline ring. The results of the two series indicate the existence of superior functional groups such as methoxy, fluorine, and cyano for the indenoisoquinoline 9-position. Interestingly, these functional groups coincide with established structure-activity relationships for the 11-position of camptothecin.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Morrell A,Placzek M,Parmley S,Grella B,Antony S,Pommier Y,Cushman Mdoi
10.1021/jm070307+subject
Has Abstractpub_date
2007-09-06 00:00:00pages
4388-404issue
18eissn
0022-2623issn
1520-4804journal_volume
50pub_type
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