ChemMedChem p. 1974 - 1979 (2015)
Update date:2022-08-29
Topics:
Nicolaou
Rhoades, Derek
Wang, Yanping
Totokotsopoulos, Sotirios
Bai, Ruoli
Hamel, Ernest
The design, synthesis, and biological evaluation of a series of epothilone analogues with novel side chains equipped with an amino group are described. Their design facilitates potential conjugation to selective drug delivery systems such as antibodies. Their synthesis proceeded efficiently via Stille coupling of a readily available vinyl iodide and heterocyclic stannanes. Cytotoxicity studies and tubulin binding assays revealed two of these analogues to be more potent than epothilones A-D and the anticancer agent ixabepilone, currently in clinical use. Ready for delivery: The design, synthesis and biological evaluation of several new epothilone analogues with regard to their tubulin binding affinities and their capacity to inhibit cancer cell growth are reported. The biological activities of these analogues fall within existing SARs for the epothilone family and will help guide future work toward higher potencies and conjugation with cancer-cell-specific antibodies and other delivery systems for targeted cancer chemotherapy.
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Doi:10.1021/ja01023a067
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