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Enediyne Derivatives

Summary

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.

Technology Benefits

1. Heat-liable
2. Chemically stable at room temperature
3. Easy to be handled

Technology Application

- A potential replacement of the anticancer drug enediyne

Supplementary Information

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

Industry

Disease Diagnostic/Treatment

Sub Group

Cancer/Tumor

Application Date

21 Jul 2000

Application No.

US 09/621517

Patent Information

US 6391916

ID No.

TTC.PA.123, TTC.PA.124

Country/Region

Hong Kong

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