申请人:FARMITALIA CARLO ERBA S.r.l.
公开号:EP0246868A1
公开(公告)日:1987-11-25
Distamycin A analogs of the following formula (I):
wherein
n is 2,3 or 4;
A is a divalent radical chosen from
and -Het-, wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole, the said radical being unsubstituted or substituted by one or more substituents chosen from C1-C6 alkyl, C1-C6 alkoxy, cyano and trifluoromethyl;
and either one of R, and R2 is hydrogen and the other is
a) a group
in which R3 is C1-C6 alkvl unsubstituted or substituted by halogen atoms; phenyl; or cyclohexyl; or
b) a group -CO-(CH2)m-R4 in which m is zero, 1,2 or 3 and R4 is hydrogen, halogen, hydroxy, aziridinyl or oxiranyl; or R, and R2 are the same and they are both hydrogen or both a C1-C6 alkyl group unsubstituted or substituted by halogen, hydroxy or C1-C6 alkoxy; and the pharmaceutically acceptable salts thereof; are antitumor and antiviral agents.
下式(I)的地达霉素 A 类似物:
其中
n 是 2、3 或 4;
A 是二价基,选自
和-Het-,其中 Het 是五原子或六原子杂环,吡咯除外,所述基团未被取代或被一个或多个选自 C1-C6 烷基、C1-C6 烷氧基、氰基和三氟甲基的取代基取代;
R 和 R2 中的一个是氢,另一个是
a) 基团
其中 R3 是未取代或被卤素原子取代的 C1-C6 烷基;苯基;或环己基;或
b) 一个基团-CO-(CH2)m-R4,其中 m 为零、1、2 或 3,R4 为氢、卤素、羟基、氮杂环丁基或环氧乙烷基;或 R 和 R2 相同,且它们都是氢或都是未被卤素、羟基或 C1-C6 烷氧基取代或取代的 C1-C6 烷基;及其药学上可接受的盐;它们都是抗肿瘤和抗病毒药。