Some new paclitaxel analogs, modified at ring C, - namely the 7-alpha-mesylate, 7-deoxy-7-alpha-amino, 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-5 alpha-acetoxy-Delta(6,7)-20-O-seco and 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-6,7-epoxy-20-O-seco derivatives -are presented. The biological activity of 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-5 alpha-acetoxy-Delta(6,7)-20-O-seco, 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-5 alpha-acetoxy-6,7-epoxy-20-O-seco, 7-deoxy-7-alpha-azido, 7-deoxy-7-alpha-amino and 6,7-epoxy derivatives have been evaluated A molecular modeling study on some paclitaxel derivatives has been done in an attempt to rationalize the difference in biological activity.
Menichincheri, M., Botta, M., Ceccarelli, W., Ciomei, M., Corelli, F., Danello, M., et al. (1995). SYNTHESIS AND MOLECULAR MODELING OF TAXANES MODIFIED AT RING-C. MEDICINAL CHEMISTRY RESEARCH, 5(7), 534-555.
SYNTHESIS AND MOLECULAR MODELING OF TAXANES MODIFIED AT RING-C
BOTTA, MAURIZIO;CORELLI, FEDERICO;TAFI, ANDREA;
1995-01-01
Abstract
Some new paclitaxel analogs, modified at ring C, - namely the 7-alpha-mesylate, 7-deoxy-7-alpha-amino, 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-5 alpha-acetoxy-Delta(6,7)-20-O-seco and 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-6,7-epoxy-20-O-seco derivatives -are presented. The biological activity of 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-5 alpha-acetoxy-Delta(6,7)-20-O-seco, 4-deacetoxy-4 alpha-hydroxy-4 beta-hydroxymethyl-5 alpha-acetoxy-6,7-epoxy-20-O-seco, 7-deoxy-7-alpha-azido, 7-deoxy-7-alpha-amino and 6,7-epoxy derivatives have been evaluated A molecular modeling study on some paclitaxel derivatives has been done in an attempt to rationalize the difference in biological activity.
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https://hdl.handle.net/11365/33984
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