Scaffold targeting drug-resistant colon cancers.

Abstract

We have identified five derivatives of the natural product sansalvamide A that are potent against multiple drug-resistant colon cancer cell lines. These analogs share no structural homology to current colon cancer drugs, are cytotoxic at levels on par with existing drugs treating other cancers, and demonstrate selectivity for drug-resistant colon cancer cell lines over noncancerous cell lines. Thus, we have established sansalvamide A as a privileged structure for treating multiple drug-resistant colon cancers.

• Authors: Katerina Otrubova, Kathleen L McGuire, Shelli R McAlpine
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 50 Issue 9 Pg. 1999-2002 (May 03 2007) ISSN: 0022-2623 [Print] United States
• PMID: 17411027 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Depsipeptides
• sansalvamide A

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Colonic Neoplasms
• Depsipeptides (chemical synthesis, chemistry, pharmacology)
• Drug Resistance, Neoplasm
• Drug Screening Assays, Antitumor
• Humans
• Structure-Activity Relationship