Cytotoxic activities of jadomycin B and five new jadomycin derivatives against four cancer cell lines (HepG2, IM-9, IM-9/Bcl-2 and H460) were evaluated. Jadomycin S was most potent against HepG2, IM-9 and IM-9/Bcl-2 while jadomycin F was most potent against H460. Their potencies correlated with the degrees of apoptosis induced. Structure-activity-relationship analyses clearly demonstrate that the side chains of the oxazolone ring derived from the incorporated amino acids make a significant impact on biological activity. Therefore, jadomycin offers an ideal scaffold to manipulate structure and could be exploited to make many novel bioactive compounds with altered activities.
|Number of pages||4|
|Journal||Journal of Antibiotics|
|State||Published - Jul 2005|
Bibliographical noteFunding Information:
Acknowledgments We wish to thank Professor Xiu-Fen Kou for her assistance with purification methods, Mr. Li Xiao-Ming for his assistance with LC-MS analyses and Mrs. Wang Jing for her assistance operating flow cytometry. This work was supported by start-up funding from Institute of Microbiology and Chinese Academy of Sciences to KQY, and by the NIH and the Kentucky Lung Cancer Research Foundation to JR.
- Streptomyces venezuelae
ASJC Scopus subject areas
- Drug Discovery