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Bioorg Med Chem Lett. 2006 Nov 15;16(22):5814-7. Epub 2006 Sep 8.

Separation of anti-angiogenic and cytotoxic activities of borrelidin by modification at the C17 side chain.

Author information

1
Biotica Technology Ltd, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, UK. barrie.wilkinson@biotica.com

Abstract

A set of novel borrelidin analogues have been prepared by precursor-directed biosynthesis. Structure-activity relationship analysis suggests that steric structural arrangement within the C17 side chain is important for differentiating cytotoxic and anti-angiogenic activities. A C17-cyclobutyl analogue 3 was found to have markedly increased selectivity for in vitro angiogenesis inhibition over cytotoxicity and is therefore potentially useful as an anticancer agent.

PMID:
16962775
DOI:
10.1016/j.bmcl.2006.08.073
[Indexed for MEDLINE]
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