Synthesis and Evaluation of Topoisomerase 1 Inhibitors
- Summary
- 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.
- Technology Benefits
- Increased antitumor effects compared to standard camptothecinGreater binding affinity to DNA at unique binding sites target cancer cell genomes specifically Increased stability and cellular uptakeTOP1 is a proven target for cancer therapy
- Technology Application
- Pharmecutical R&D requiring superior pharmacological properties and increased cytotoxic effectsMedical/HealthcareCancer TreatmentDrug Development
- Detailed Technology Description
- Mark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology
- Countries
- United States
- Application No.
- 7,312,228
- *Abstract
-
- *Background
- 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.
- *IP Issue Date
- Dec 25, 2007
- *IP Type
- Utility
- *Stage of Development
- Concept Developed
- *Web Links
- Purdue Office of Technology CommercializationPurdueInnovation and EntrepreneurshipMark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology
- Country/Region
- USA
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