Synthesis Of 2-O-Heteroaroyl Taxanes - Evaluation Of Microtubule Assembly Promotion And Cytotoxicity
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS(1995)
Abstract
A series of heterocyclic taxanes were synthesized and evaluated to investigate structure activity relationships at the 2-position of paclitaxel. The compounds were prepared through a regioselective deacylation, reacylation sequence of suitably protected paclitaxel. The heterocyclic substituted diterpenes were synthesized from paclitaxel in four steps in high overall yields. Evaluation of these analogues in a microtubule assembly assay and for their cytotoxicity against B16 melanoma cells illustrated that these compounds had diminished activity compared to paclitaxel.
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Key words
structure activity relationship
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