Synthesis and Evaluation of Topoisomerase 1 Inhibitors

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Unique DNA binding site specificities allow the indenoisoquinoline derivatives to target the cancer cell genome selectively inducing novel DNA cleavage patterns. The engineered molecules display improved cytotoxicity and increased inhibition of TOP1 over preexisting topoisomerase-targeted therapeutics.

Researchers at Purdue University have developed novel, non-camptothecin, indenoisoquinoline-based topoisomerase 1 (TOP1) inhibitor compounds that exhibit superior pharmacological properties and increased cytotoxic effects when compared to camptothecins. By further developing the structure-activity relationship of therapeutic compounds, researchers have designed an indenoisoquinoline molecule with increased stability, improved cellular uptake, and greater binding affinity to DNA.

Advantages:
-Increased antitumor effects compared to standard camptothecin
-Greater binding affinity to DNA at unique binding sites target cancer cell genomes specifically
-Increased stability and cellular uptake
-TOP1 is a proven target for cancer therapy

Potential Applications:
-Pharmecutical R&D requiring superior pharmacological properties and increased cytotoxic effects
Oct 14, 2005
United States
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Purdue Office of Technology Commercialization
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West Lafayette, IN 47906

Phone: (765) 588-3475
Fax: (765) 463-3486
Email: otcip@prf.org