| 摘要 |
PURPOSE: The compounds of the invention are strong cytotoxic drug, especially are effective to cells resistant to known anticancer drugs and causes apoptosis, which is important to cancer treatment, to the cells. The compounds can be administered in the form of salt by being dissolved in aqueous solvent, without the use of toxic detergents, due to their basic properties. CONSTITUTION: The invention relates to taxen derivatives produced by starting from 10-deacethyl-baccatin III, 14-hydroxy-10-deacethyl-baccatin III, 19-hydroxy-10-deacethyl-baccatin III and their ester at 13th carbon position and reacting respective 10-dehydro-derivatives with hydrazine, hydroxyl amine and their derivatives. The new compounds have pyrazoline groups at the position of 7th carbon and 9th carbon. Esters with isoserine, having functional group at the position of 3rd carbon and NH, at the position of 13th carbon have in vivo anticancer activity and cytotoxic action to nearly all human carcinoma cell lines.
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