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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

Country/Region

USA

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