Green M, Bragdon J, Rankin A
Proc Natl Acad Sci U S A. 1972 May;69(5):1294-8. doi: 10.1073/pnas.69.5.1294.
Derivatives of rifamycin-SV with substituted cyclic-amine side chains in position 3 of the ansa ring are strong inhibitors of RNA-directed DNA and DNA-directed DNA polymerase activity of RNA tumor viruses of murine, feline, and avian origin. Among 37 3-amine derivatives of rifamycin-SV that were tested, 29 3-cyclic amine derivatives were good inhibitors of the viral polymerases. Especially active were 3-piperidyl derivatives of rifamycin-SV with cyclohexyl and cyclohexylalkyl substituents. Derivatives that were effective against the viral polymerase also blocked cell transformation by the murine sarcoma virus. A DNA-directed DNA polymerase preparation from human KB cells was less sensitive to inhibition by these derivatives than the virion polymerase.
在安莎环3位带有取代环胺侧链的利福霉素-SV衍生物是鼠源、猫源和禽源RNA肿瘤病毒的RNA指导的DNA和DNA指导的DNA聚合酶活性的强抑制剂。在测试的37种利福霉素-SV的3-胺衍生物中，29种3-环胺衍生物是病毒聚合酶的良好抑制剂。利福霉素-SV的3-哌啶基衍生物与环己基和环己基烷基取代基特别具有活性。对病毒聚合酶有效的衍生物也能阻断鼠肉瘤病毒引起的细胞转化。来自人KB细胞的DNA指导的DNA聚合酶制剂对这些衍生物的抑制作用比病毒体聚合酶更不敏感。
