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

  • Bioorg Med Chem Lett. 2011 Aug 1;21(15):4462-4. doi: 10.1016/j.bmcl.2011.06.005.
Shashikanth Ponnala  1 ,  Sandeep Chaudhary ,  Antonio González-Sarrias ,  Navindra P Seeram ,  Wayne W Harding
Affiliations
  • 1. Chemistry Department, Hunter College, CUNY, New York, NY 10065, USA.
PMID: 21724394 DOI: 10.1016/j.bmcl.2011.06.005
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.

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