Cytotoxic activities of new jadomycin derivatives.

Abstract

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.

• Authors: Jian-Ting Zheng, Uwe Rix, Lixia Zhao, Cynthia Mattingly, Val Adams, Quan Chen, Jürgen Rohr, Ke-Qian Yang
• Journal: The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 58 Issue 6 Pg. 405-8 (Jun 2005) ISSN: 0021-8820 [Print] England
• PMID: 16156517 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antibiotics, Antineoplastic
• Isoquinolines
• jadomycin B

Topics

• Antibiotics, Antineoplastic (chemistry, toxicity)
• Apoptosis (drug effects)
• Cell Line, Tumor
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Humans
• Isoquinolines (chemistry, toxicity)
• Streptomyces (drug effects)
• Structure-Activity Relationship