Cytotoxicity of aporphines in human colon cancer cell lines HCT-116 and Caco-2: an SAR study.

Abstract

A series of synthetic aporphine derivatives structurally related to domesticine and nantenine (ring A, N6 and ring C truncated analogs), was evaluated in MTS cytotoxicity assays against the human colon cancer cell lines, HCT-116 and Caco-2. In general, the C1 position of ring A is tolerant of alkoxy substituents as well as a benzoyl ester functionality. Other modifications evaluated resulted in a decrease in cytotoxic activity. The most potent compounds identified had IC(50) values in the range 23-38 μM, comparable to the known cytotoxic agent, etoposide.

• Authors: Shashikanth Ponnala, Sandeep Chaudhary, Antonio González-Sarrias, Navindra P Seeram, Wayne W Harding
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 21 Issue 15 Pg. 4462-4 (Aug 01 2011) ISSN: 1464-3405 [Electronic] England
• PMID: 21724394 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
• Copyright: Copyright © 2011 Elsevier Ltd. All rights reserved.

Chemical References

• Aporphines
• domesticine
• nantenine

Topics

• Aporphines (chemistry, therapeutic use, toxicity)
• Caco-2 Cells
• Colonic Neoplasms (drug therapy)
• Drug Screening Assays, Antitumor
• HCT116 Cells
• Humans
• Structure-Activity Relationship