Author/Authors :
Barrie Wilkinson، نويسنده , , Matthew A. Gregory، نويسنده , , Steven J. Moss، نويسنده , , Isabelle Carletti، نويسنده , , Rose M. Sheridan، نويسنده , , Andrew Kaja، نويسنده , , Michael Ward، نويسنده , , Carlos Olano، نويسنده , , Carmen Mendez، نويسنده , , José A. Salas، نويسنده , , Peter F. Leadlay، نويسنده , , Rob vanGinckel، نويسنده , , Mingqiang Zhang، نويسنده ,
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.
Keywords :
Polyketide , Borrelidin , Angiogenesis inhibitor , biosynthetic engineering
