申请人:SUMITOMO CHEMICAL COMPANY, LIMITED
公开号:EP0092963A1
公开(公告)日:1983-11-02
A compound of the formula
wherein X' is a free or an esterified carboxyl group, or a group of the formula:
(Ra and Rb are each independently a hydrogen atom, a C1-C4 alkyl group, a C3-C7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom of a C,-C4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group), Y is a group of the formula:
(R6 is a hydrogen atom or a C1-C4 alkyl group) or
(R6 is as defined above), R' is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R2 is a hydrogen atom or R' and R2, when taken together, mean a single linkage to form a double bond between the carbon atoms which they are linked, R3 is a hydroxyl group or a protected hydroxyl group, R4 is a hydrogen atom or a C,-C4 alkyl group, R5 is a hydrogen atom, a C3 - C8 alkynyl group, a C3-C8 alkenyl group, a C1-C8 alkyl group, a C3-C7 cycloalkyl group, a hydroxy C1-C8 alkyl group or a group of the formula: -(CH2)m-B (m is 1 or 2 and B is C,-C4 alkoxy, a C3-C7 cycloalkyl, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C1-C4 alkyl group, a trifluoromethyl group or a C1-C4 alkoxy group), n is 2 or 3; or a non-toxic pharmaceutically acceptable salt thereof has strong anti- cancer activity and is useful in treatment of a cancer.
式中的化合物
其中 X'是游离的或酯化的羧基,或式中的基团:
(Ra和Rb各自独立地为氢原子、C1-C4烷基、C3-C7环烷基、苄基、苯基、被C,-C4烷基的卤素原子取代的苯基,或当与相连的相邻氮原子合在一起时,它们代表5至7个成员的饱和杂环基团),Y为式中的基团:
(R6 是氢原子或 C1-C4 烷基)或
(R6 如上定义),R'是氢原子、羟基或受保护的羟基,R2 是氢原子或 R'和 R2 合在一起时表示单链,在它们所连接的碳原子之间形成双键、R3 是羟基或受保护的羟基,R4 是氢原子或 C,-C4烷基,R5 是氢原子、C3-C8 炔基、C3-C8 烯基、C1-C8 烷基、C3-C7 环烷基、羟基 C1-C8 烷基或式中的基团:-(
CH2)m-B(m 为 1 或 2,B 为 C、-C4 烷氧基、C3-C7 环烷基、或任选被卤素原子、C1-C4 烷基、三
氟甲基或 C1-C4 烷氧基取代的苯基或苯氧基),n 为 2 或 3;或其无毒药学上可接受的盐,具有很强的抗癌活性,可用于治疗癌症。