Modification of marine natural product ningalin B and SAR study lead to potent P-glycoprotein inhibitors.

Abstract

In this study, new marine ningalin B analogues containing a piperazine or a benzoloxy group at ring C have been synthesized and evaluated on their P-gp modulating activity in human breast cancer and leukemia cell lines. Their structure-activity relationship was preliminarily studied. Compounds 19 and 20 are potent P-gp inhibitors. These two synthetic analogues of permethyl ningalin B may be potentially used as effective modulators of P-gp-mediated drug resistance in cancer cells.

• Authors: Chao Yang, Iris L K Wong, Wen Bin Jin, Tao Jiang, Larry M C Chow, Sheng Biao Wan
• Journal: Marine drugs (Mar Drugs) Vol. 12 Issue 10 Pg. 5209-21 (Oct 17 2014) ISSN: 1660-3397 [Electronic] Switzerland
• PMID: 25329704 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• ATP Binding Cassette Transporter, Subfamily B, Member 1
• Antineoplastic Agents
• Biological Products
• Heterocyclic Compounds, 3-Ring
• Piperazines
• ningalin B
• Piperazine

Topics

• ATP Binding Cassette Transporter, Subfamily B, Member 1 (antagonists & inhibitors)
• Antineoplastic Agents (chemistry, pharmacology)
• Biological Products (chemistry, pharmacology)
• Breast Neoplasms (drug therapy)
• Cell Line, Tumor
• Drug Resistance, Multiple (drug effects)
• Drug Resistance, Neoplasm (drug effects)
• Female
• Heterocyclic Compounds, 3-Ring (chemistry, pharmacology)
• Humans
• K562 Cells
• Leukemia (drug therapy)
• Piperazine
• Piperazines (chemistry, pharmacology)
• Structure-Activity Relationship