Potent and selective inhibition of human cytochrome P450 3A4 by seco-pancratistatin structural analogs |
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| Authors: | James McNulty Jerald J. Nair Mohini Singh Denis J. Crankshaw Alison C. Holloway |
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| Affiliation: | 1. Department of Chemistry and Chemical Biology, McMaster University, 1280 Main Street West, Hamilton, Ont., Canada L8S 4M1;2. Department of Obstetrics and Gynecology, McMaster University, 1200 Main Street West, Hamilton, Ont., Canada L8N 3Z5 |
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| Abstract: | seco-Derivatives of the anticancer agent pancratistatin bearing the 2S,3S,4S,5S configuration were accessed via a novel, highly diastereoselective anti-aldol reaction. Structure–activity relationships reveal important insights into the seco-pancratistatin pharmacophore as a potent and selective inhibitor of human cytochrome P450 3A4 (CYP3A4), and highlight features of concern in advancing a potent, selective anticancer agent in the pancratistatin series. |
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