申请人:Zaidanhojin Biseibutsu
Kagaku Kenkyukai
公开号:EP0238868A2
公开(公告)日:1987-09-30
The present invention provides new physiological active substance erbstatin analogue compounds of a general formula (I), which have excellent tyrosine-specific protein-kinase inhibitory activity, antitumor activity and antimicrobial activity.
in which R1 represents a hydrogen atom, a lower alkanoyl group or a lower alkyl group; n represents a positive integer of
1 to3;
X represents a hydrogen atom or a halogen atom;
Y represents a group of formula -CH=CH-NC, -CH=CH-NHR2 or-CH2-CH2-NHR2
(where R2 represents a formyl group or a lower alkanoyl group; with the exception of the cases where X is hydrogen atom, (R10)n group is 2,5-dihydroxy group and Y is -CH=CH-NHCHO or-CH2-CH2-NHCHO).
The present invention further provides a tyrosine-specific protein-kinase inhibitor, tumoricide or bactericide containing at least one compound of the said formula (I).
本发明提供了通式(I)的新型生理活性物质厄贝沙坦类似物化合物,其具有优异的酪氨酸特异性蛋白激酶抑制活性、抗肿瘤活性和抗菌活性。
其中,R1 代表氢原子、低级烷酰基或低级烷基;n 代表以下的正整数
1至3的正整数;
X 代表氢原子或卤素原子;
Y 代表式-CH=CH-NC、-CH=CH-NHR2 或-CH2-CH2-NHR2 的基团
(其中 R2 代表甲酰基或低级烷酰基;X 为氢原子、(R10)n 基团为 2,5-二羟基和 Y 为 -CH=CH-NHCHO 或-CH2-CH2-NHCHO 的情况除外)。
本发明进一步提供了一种含有至少一种所述式(I)化合物的酪氨酸特异性蛋白激酶抑制剂、杀瘤剂或杀菌剂。