Triheterocyclic peptides capable of binding the minor and major grooves
of DNA
    21.
    发明授权
    Triheterocyclic peptides capable of binding the minor and major grooves of DNA 失效
    能够结合DNA的小槽和主槽的三重杂环肽

    公开(公告)号:US5698674A

    公开(公告)日:1997-12-16

    申请号:US226934

    申请日:1994-04-13

    CPC分类号: C07D207/34

    摘要: The present invention provides a triheterocyclic peptide having first, second, and third 5-member heterocyclic moieties having the following formula CR.sub.3 CONH--Q.sup.1 --CONH--Q.sup.2 --CONH--Q.sup.3 -CONH--(CR.sub.3).sub.S --B, wherein Q.sup.1 is selected from a group consisting of: ##STR1## wherein Q.sup.2 is selected from a group consisting of: ##STR2## wherein Q.sup.3 is selected from a group consisting of: ##STR3## wherein at least one of A and Z is other than C; wherein A is C, N, O, or S; wherein B is N(CR.sub.3).sub.n or C(NH.sub.2).sub.2 ; wherein n is an integer from 2 to 10; wherein P is H, a lower alkyl or a halogen; wherein Q1, Q2, and Q3 are the same or different; wherein R is H, a lower alkyl group; wherein S is an integer from 1 to 10; wherein X' represents CR.sub.3, (CR.sub.2).sub.n --NRY, or (CR.sub.2).sub.n --CR.sub.2 Y; wherein X" represents CR.sub.3, (CR.sub.2).sub.n --NRY, or (CR.sub.2).sub.n --CR.sub.2 Y; wherein X'" represents CR.sub.3, (CR.sub.2).sub.n --NRY, or (CR.sub.2).sub.n --CR.sub.2 Y; wherein Y is a polyamine group, and wherein Z is C or N; wherein at least one of X', X", or X'" is other than CR.sub.3.

    摘要翻译: 本发明提供具有具有下式CR 3 CONH-Q1-CONH-Q2-CONH-Q3-CONH-(CR 3)SB的第一,第二和第三个5元杂环部分的三杂环肽,其中Q1选自 其中Q 2选自:其中Q 3选自:其中A和Z中的至少一个不是C;其中Q 3选自: 其中A是C,N,O或S; 其中B是N(CR 3)n或C(NH 2)2; 其中n是2至10的整数; 其中P是H,低级烷基或卤素; 其中Q1,Q2和Q3相同或不同; 其中R是H,低级烷基; 其中S为1至10的整数; 其中X'代表CR3,(CR2)n-NRY或(CR2)n-CR2Y; 其中X“表示CR3,(CR2)n-NRY或(CR2)n-CR2Y; 其中X“表示CR 3,(CR 2)n-NRY或(CR 2)n-CR 2 Y; 其中Y是多胺基团,并且其中Z是C或N; 其中X',X“或X”'中的至少一个不是CR 3。