Synthesis and Evaluation of Topoisomerase 1 Inhibitors
- 總結
- 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.
- 技術優勢
- 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
- 技術應用
- Pharmecutical R&D requiring superior pharmacological properties and increased cytotoxic effectsMedical/HealthcareCancer TreatmentDrug Development
- 詳細技術說明
- Mark CushmanPurdue Medicinal Chemistry and Molecular Pharmacology
- *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
- 國家
- United States
- 申請號碼
- 7,312,228
- 國家/地區
- 美國
欲了解更多信息，請點擊 這裡
