丝裂霉素类抗生素。7-甲氧基-1-(N-吡咯烷基)丝裂蒽醌及其甲碘化物的合成。

Mitomycin antibiotics. Synthesis of 7-methoxy-1-(N-pyrrolidino)mitosene and its methiodide.

作者信息

Mott J, Remers W A

出版信息

J Med Chem. 1978 May;21(5):493-5. doi: 10.1021/jm00203a020.

Abstract

7-Methoxy-1-(N-pyrrolidino)mitosene and its methiodide were synthesized. The latter compound was a potential bifunctional alkylating agent because of its two good leaving groups appropriately situated with respect to the indoloquinone chromophore. However, it was inactive in bacteriophage induction and P388 murine leukemia assays. Both compounds showed antibacterial activity in culture, and the former compound was very weakly active in inducing lysogenic bacteriophage.

摘要

合成了7-甲氧基-1-(N-吡咯烷基)米托蒽醌及其甲碘化物。后一种化合物是一种潜在的双功能烷基化剂，因为其两个良好的离去基团相对于吲哚醌发色团的位置适当。然而，它在噬菌体诱导和P388小鼠白血病试验中无活性。两种化合物在培养物中均表现出抗菌活性，前一种化合物在诱导溶源性噬菌体方面活性非常弱。