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

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

  • Bioorg Med Chem Lett. 2006 Nov 15;16(22):5814-7. doi: 10.1016/j.bmcl.2006.08.073.
Barrie Wilkinson 1,  Matthew A Gregory,  Steven J Moss,  Isabelle Carletti,  Rose M Sheridan,  Andrew Kaja,  Michael Ward,  Carlos Olano,  Carmen Mendez,  José A Salas,  Peter F Leadlay,  Rob vanGinckel,  Ming-Qiang Zhang
Affiliations

Affiliation

  • 1 Biotica Technology Ltd, Chesterford Research Park, Little Chesterford, Essex CB10 1XL, UK. [email protected]
PMID: 16962775 DOI: 10.1016/j.bmcl.2006.08.073
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.

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