| 摘要 |
PURPOSE:To obtain the subject new derivative having anti-tumor activity, a strong in vitro proliferation inhibiting activity against mouse lymphatic leukemia cell and low toxicity and useful as a tumor treating agent, etc., by deriving from okadaic acid separated from a porifera. CONSTITUTION:The objective new okadaic acid derivative of formula II (R is amine residue of oligopeptide) having anti-tumor activity and low toxicity and useful as a tumor treating agent, etc., is obtained by derivatizing okadaic acid of formula I (Me is methyl) separated from Halichondria okada Kadota of a porifera to its p-nitrophenyl ester, adding glycylglycine, etc., to the ester, reacting the mixture under stirring in the presence of pyridine, triethylamine and water for 24 hours, subjecting the reaction solution to vacuum concentration after the completion of the reaction and purifying the concentrated product through silica gel chromatography. |
