CHEMOTHERAPEUTIC POLYMER ⅩⅦ. THE SYNTHESIS AND ANTITUMOR ACTIVITY OF POLYPHOSPHATES CONTAINING BOTH NUCLEIC ACID BASE AND NITROGEN MUSTARD

【摘要】 <正> Seven new polyphosphates containing both nucleic acid base and nitrogen mustard were preparedby reacting the monomers, i.e. 1,3-dihydroxyalkyl-5-fluorouracil(II_{a.,b, g}), 1,3-dihydroxyalkyluracil(II_c,d) and 1, 3-dihydroxyalkylthymine (II_e,f) with W, N,N-bis（2-chloroethyl）phosphoramide dichlo-ride （I）. The monomers and polymers were characterized by ¹H-NMR, IR spectra and elementalanalysis. All of the polymers obtained are soluble in water. The antitumor activity of some of thesepolymers were tested against Ehrlish Ascites in mice. The results showed that the polyphosphatescontaining both 5-fluorouracil and nitrogen mustard exhibit lower toxicity and higher antitumor ac-tivity. The inhibition ratio of the polymer （III_a） is 66%.更多还原

【Abstract】 Seven new polyphosphates containing both nucleic acid base and nitrogen mustard were preparedby reacting the monomers, i.e. 1,3-dihydroxyalkyl-5-fluorouracil(II_{a.,b, g}), 1,3-dihydroxyalkyluracil(II_c,d) and 1, 3-dihydroxyalkylthymine (II_e,f) with W, N,N-bis（2-chloroethyl）phosphoramide dichlo-ride （I）. The monomers and polymers were characterized by ¹H-NMR, IR spectra and elementalanalysis. All of the polymers obtained are soluble in water. The antitumor activity of some of thesepolymers were tested against Ehrlish Ascites in mice. The results showed that the polyphosphatescontaining both 5-fluorouracil and nitrogen mustard exhibit lower toxicity and higher antitumor ac-tivity. The inhibition ratio of the polymer （III_a） is 66%.更多还原