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

ZHOU Nianen; CHEN Qusheng; ZHUO Renxi

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

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- CHEMOTHERAPEUTIC POLYMER ⅩⅦ. THE SYNTHESIS AND ANTITUMOR ACTIVITY OF POLYPHOSPHATES CONTAINING BOTH NUCLEIC ACID BASE AND NITROGEN MUSTARD
- Vol. 4, Issue 4, Pages: 316-321(1986)
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- Published：20 December 1986
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ZHOU Nianen, CHEN Qusheng, ZHUO Renxi. CHEMOTHERAPEUTIC POLYMER ⅩⅦ. THE SYNTHESIS AND ANTITUMOR ACTIVITY OF POLYPHOSPHATES CONTAINING BOTH NUCLEIC ACID BASE AND NITROGEN MUSTARD[J]. 1986, 4(4): 316-321.
DOI：

ZHOU Nianen, CHEN Qusheng, ZHUO Renxi. CHEMOTHERAPEUTIC POLYMER ⅩⅦ. THE SYNTHESIS AND ANTITUMOR ACTIVITY OF POLYPHOSPHATES CONTAINING BOTH NUCLEIC ACID BASE AND NITROGEN MUSTARD[J]. 1986, 4(4): 316-321. DOI：

摘要

Seven new polyphosphates containing both nucleic acid base and nitrogen mustard were preparedby reacting the monomers

i.e. 1

3-dihydroxyalkyl-5-fluorouracil(IIa.

3-dihydroxyalkyluracil(IIc

d) and 1

3-dihydroxyalkylthymine (IIe

f) with W

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 polyphosphates containing both 5-fluorouracil and nitrogen mustard exhibit lower toxicity and higher antitumor activity.The inhibition ratio of the polymer(Ⅲa) is 66%.

Abstract

Seven new polyphosphates containing both nucleic acid base and nitrogen mustard were preparedby reacting the monomers

i.e. 1

3-dihydroxyalkyl-5-fluorouracil(IIa.

3-dihydroxyalkyluracil(IIc

d) and 1

3-dihydroxyalkylthymine (IIe

f) with W

N-bis(2-chloroethyl)phosphoramide dichlo-ride (I). The monomers and polymers were characterized by 1H-NMR

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