Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 15, Pages 4462-4464Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.005
Keywords
Aporphine; Nantenine; Cytotoxic; HCT-116; Caco-2
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Funding
- National Center for Research Resources (NCRR) of the National Institutes of Health (NIH) [RR03037]
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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 IC50 values in the range 23-38 mu M, comparable to the known cytotoxic agent, etoposide. (C) 2011 Elsevier Ltd. All rights reserved.
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