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腺苷脱氨酶抑制剂2'-脱氧助间型霉素增强腺苷类似物的生物活性

Enhancement of the biological activity of adenosine analogs by the adenosine deaminase inhibitor 2'-deoxycoformycin.

作者信息

Adamson R H, Zaharevitz D W, Johns D G

出版信息

Pharmacology. 1977;15(1):84-9. doi: 10.1159/000136666.

Abstract

The potent adenosine deaminase inhibitor 2'-deoxycoformycin ((R)-3-(2-deoxy-beta-D-erythropentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol) inhibits the enzymic inactivation and potentiates the cytotoxic activity of a variety of adenosine analogs in the P388 murine leukemia cell culture system. The activity of all seven adenosine analogs examined was enhanced by 2'-deoxycoformycin with the exception of tubercidin (7-deaza-adenosine) which is not a substrate for the deaminase. In vivo, 2'-deoxy-coformycin potentiated the antineoplastic activity of 9-beta-D-xylofuranosyladenine in mice with P388 murine leukemia.

摘要

强效腺苷脱氨酶抑制剂2'-脱氧助间型霉素((R)-3-(2-脱氧-β-D-赤藓戊呋喃糖基)-3,6,7,8-四氢咪唑并[4,5-d][1,3]二氮杂卓-8-醇)在P388小鼠白血病细胞培养系统中可抑制多种腺苷类似物的酶促失活,并增强其细胞毒性活性。除了不是脱氨酶底物的杀结核菌素(7-脱氮腺苷)外,所检测的所有七种腺苷类似物的活性均因2'-脱氧助间型霉素而增强。在体内,2'-脱氧助间型霉素可增强9-β-D-木糖呋喃糖基腺嘌呤对患有P388小鼠白血病的小鼠的抗肿瘤活性。

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