Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay.
The indenoisoquinolines are a novel class of non-camptothecin topoisomerase I (Top1) inhibitors whose mechanism of action involves trapping the covalent complex formed between DNA and Top1 during cellular processes. As an ongoing evaluation of the indenoisoquinolines for Top1 inhibition and anticancer activity, indenoisoquinoline analogs have been screened in the National Cancer Institute's hollow fiber assay (HFA). Some of the derivatives demonstrated significant activity at intraperitoneal and subcutaneous fiber placement sites, along with net cancer cell kill in one or more cell lines.
Morrell
Andrew
A
Department of Medicinal Chemistry and Molecular Pharmacology and the Purdue Cancer Center, School of Pharmacy and Pharmaceutical Sciences, Purdue University, West Lafayette, IN 47907, USA.
Jayaraman
Muthusamy
M
Nagarajan
Muthukaman
M
Fox
Brian M
BM
Meckley
Marintha Rae
MR
Ioanoviciu
Alexandra
A
Pommier
Yves
Y
Antony
Smitha
S
Hollingshead
Melinda
M
Cushman
Mark
M
D000970:Antineoplastic Agents / Q000494:pharmacology*; D001681:Biological Assay / Q000379:methods; D002166:Camptothecin / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor / Q000379:methods; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007546:Isoquinolines / Q000737:chemistry*; D008956:Models, Chemical; D059004:Topoisomerase I Inhibitors
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007546:Isoquinolines; D059004:Topoisomerase I Inhibitors; D004247:DNA; D002166:Camptothecin