Synthesis of 2-methyl N10-substituted acridones as selective inhibitors of multidrug resistance (MDR) associated protein in cancer cells.

Abstract

A series of N10-substituted-2-methyl acridone derivatives are synthesized and are examined for its ability to reverse P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in breast cancer cell lines MCF-7 and MCF-7/Adr. The structural requirement of in-vitro anti-cancer and reversal of drug resistance are studied. The results showed that compound 16 with four carbon spacer exhibited promising in-vitro anti-cancer and reversal of drug resistance in comparison to the other analogues.

• Authors: Y C Mayur, Osman Ahmad, V V S Rajendra Prasad, M N Purohit, N Srinivasulu, S M Shanta Kumar
• Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) (Med Chem) Vol. 4 Issue 5 Pg. 457-65 (Sep 2008) ISSN: 1573-4064 [Print] Netherlands
• PMID: 18782042 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• ATP Binding Cassette Transporter, Subfamily B, Member 1
• Acridones
• Antineoplastic Agents
• Multidrug Resistance-Associated Proteins

Topics

• ATP Binding Cassette Transporter, Subfamily B, Member 1 (metabolism)
• Acridones (chemical synthesis, pharmacology)
• Antineoplastic Agents (chemical synthesis, pharmacology)
• Breast Neoplasms (metabolism, pathology)
• Cell Line, Tumor (drug effects, pathology)
• Drug Resistance, Neoplasm
• Humans
• Models, Chemical
• Multidrug Resistance-Associated Proteins (antagonists & inhibitors)