Compounds which are prodrugs of triptolide or its derivatives, containing an amino acid or oligopeptide moiety, are used for anticancer or immunosuppressive treatment. The compounds are of the structure:
1
where X
1
is OH or OR
1
, and X
2
and X
3
are independently OH, OR
1
or H, with the proviso that at least one of X
1
, X
2
and X
3
is OR
1
, and at least one of X
2
and X
3
is H; and R
1
, is selected from the group consisting of:
2
(b): C(═O)CHY-NHP
1
(c): C(═O)CH(NHP
1
)—(CH
2
)
m
—C(═O)OP
2
(d): C(═O)(CH
2
)
n
—CH(NHP
1
)—C(═O)OP
2
and
(e): [C(═O)CHY—NH]
Z
—C(═O)CHY—NHP
1
;
where Y is a side chain of a naturally occurring amino acid or a one- or two-carbon homolog thereof; P
1
is selected from the group consisting of H, C(═O)OR
2
, and C(═O)R
3
, where each of R
2
and R
3
is independently H, alkyl, alkenyl, aryl, or aralkyl; m is an integer from 0-5; n is an integer from 0-5; z is an integer from 2-10; and P
2
is selected from the group consisting of H, alkyl, alkenyl, aryl, and aralkyl.
作为三苯甲酰或其衍
生物的原药,含有
氨基酸或寡肽分子的化合物可用于抗癌或免疫抑制治疗。这些化合物的结构如下
1
其中 X
1
是 OH 或 OR
1
和 X
2
和 X
3
独立地为 OH、OR
1
或 H,但条件是 X
1
, X
2
和 X
3
为 OR
1
中的至少一个
2
和 X
3
为 H;以及 R
1
选自以下组成的组
2
(b):C(═O)CHY-NHP
1
(c):C(═O)CH(NHP
1
)-(CH
2
)
m
-C(═O)OP
2
(d):C(═O)(CH
2
)
n
-CH(NHP
1
)-C(═O)OP
2
和
(e): [C(═O)CHY-NH]
Z
-C(═O)CHY-NHP
1
;
其中 Y 是天然
氨基酸的侧链或其单碳或双碳同源物;P
1
选自 H、C(═O)OR
2
和 C(═O)R
3
其中每个 R
2
和 R
3
独立地为 H、烷基、烯基、芳基或芳烷基;m 为 0-5 的整数;n 为 0-5 的整数;z 为 2-10 的整数;以及 P
2
选自由 H、烷基、烯基、芳基和芳烷基组成的组。