Enediyne Derivatives
A novel class of synthetic substances that exhibits DNA cleavage and anticancer activity is discovered. Enediyne is a well-known anticancer agent. Mechanistic study on the new invention confirms that these synthetic substances are converted into enediynes under physiological condition and then deliver enediyne-like biological activity. Compared with enediyne, these substances possess higher chemical stability at room temperature and can therefore be used as enediyne prodrugs. Several synthetic processes were developed for these substances and their DNA cleavage capability and their cytotoxicity against cancer cell lines were evaluated. The results confirm that the substances are of potential value for developing into novel anticancer agents.
1. Heat-liable
2. Chemically stable at room temperature
3. Easy to be handled
- A potential replacement of the anticancer drug enediyne
Patent Number: US6391916B1
Application Number: US2000621517A
Inventor: Dai, Wei Min | Wu, Anxin | Lee, Yuk Ha | Hamaguchi, Wataru | Nishimoto, Sei ichi | Zhou, Ling | Ishii, Atsushi
Priority Date: 21 Jul 2000
Priority Number: US6391916B1
Application Date: 21 Jul 2000
Publication Date: 21 May 2002
IPC Current: C07C003521 | C07C0043188 | C07C004323 | C07C006900 | C07C0069013 | C07C006924 | C07C0069708 | C07C0069712 | C07C006992 | C07D030779 | C07F000718
US Class: 514529 | 514416 | 514443 | 514465 | 514532 | 514543 | 514546 | 514548 | 514552 | 514719 | 514729 | 514730 | 548490 | 548491 | 549049 | 549058 | 549462 | 560187 | 560188 | 568659 | 568660
Assignee Applicant: The Hong Kong University of Science & Technology
Title: Enediyne derivatives
Usefulness: Enediyne derivatives
Summary: Used for cleaving DNA or degrading or modulating proteins useful for treating cancer or inhibiting microbial growth.
Novelty: New cyclodeca-1,5-diyne compounds useful for treating cancer or inhibiting microbial growth
診斷/治療
癌症/腫瘤
21 Jul 2000
US 6391916
TTC.PA.123, TTC.PA.124
香港
