Synthesis and Evaluation of Topoisomerase 1 Inhibitors
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.
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
Pharmecutical R&D requiring superior pharmacological properties and increased cytotoxic effectsMedical/HealthcareCancer TreatmentDrug Development
Mark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology
United States
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美国
