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Synthesis and antineoplastic activity of mitosene analogues of the mitomycins.

Abstract：

:A series of 1-substituted mitosene analogues of the mitomycin antitumor antibiotics was prepared by total synthesis and screened for activity against P388 leukemia in mice. In general, analogues with moderately good leaving groups (mostly esters) at the 1 position were active, whereas analogues without such substituents were inactive or barely active. These results lend support to the idea that mitosenes with leaving groups at position 1 are capable of bifunctional alkylation of DNA in a manner similar to that of mitomycin C. The most active mitosenes were equal in potency (minimum effective dose) to a corresponding aziridinomitosene, but they were less effective in prolonging life span.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Hodges JC,Remers WA,Bradner WT

doi

10.1021/jm00142a013

subject

Has Abstract

pub_date

1981-10-01 00:00:00

pages

1184-91

issue

10

eissn

0022-2623

issn

1520-4804

journal_volume

24

pub_type

杂志文章

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