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    Synthesis and antitumor activity of 2,4,5-trisubstituted-pyrrolo2,3-d]-pyrimidine nucleosides
    72.
    发明授权
    Synthesis and antitumor activity of 2,4,5-trisubstituted-pyrrolo2,3-d]-pyrimidine nucleosides 失效
    2,4,5-三取代 - 吡咯并[b 2,3-d] {9 - 嘧啶核苷的合成和抗肿瘤活性

    公开(公告)号：US4140851A

    公开(公告)日：1979-02-20

    申请号：US853490

    申请日：1977-11-21

    Applicant: Leroy B. Townsend

    Inventor： Leroy B. Townsend

    IPC: C07H19/14 ,  C07H17/00 ,  A61K31/70 ,  C07H19/06

    CPC classification number: C07H19/14 ,  Y10S514/908

    Abstract: Certain trisubstituted pyrrolopyrimidine nucleosides are prepared from toyocamycin and have shown antitumor activity against L1210 and P388 murine leukemia. The particular compounds of interest are selected from the following structural formula: ##STR1## where X is haloY is halo; --NH.sub.2 ; --SH, --SR (where R is lower alkyl, benzyl); --OR (where OR is methoxy or alkoxy or where alk is C1-C6); amino (where the amino is --NH.sub.2, -alkyl amino or -dialkyl amino and alkyl is C1-C6); gamma gamma dimethyl allyl amino; benzyl amino; phenyl amino; selenoZ is CN; CXNH.sub.2 where X is .dbd.0, .dbd.S, or .dbd.Se, .dbd.NH, .dbd.NHNH.sub.2, .dbd.NOH. OR Z is = --CH.sub.2 NH.sub.2, --COR.dbd.NHRib.dbd..beta.-D-ribofuranosylPreferred members of this group of compounds are shown by the following structural formula: ##STR2## where X is ClY is Cl or NH.sub.2Z is CN, CONH.sub.2, or C.dbd.NOH--NH.sub.2These compounds are further identified as NSC #145387 (Compound 5) ##STR3## NSC #177369 (Compound 6) ##STR4## NSC #182864 (Compound 8) ##STR5## NSC #180526 (Compound 10) ##STR6## These compounds at dosages of 13 - 200 mg/kg of body weight administered every other day on the standard six-day schedule showed activity against both L1210 and P388 murine leukemia (Protocol 11, National Institutes of Health, November 11, 1972).

    Abstract translation: 某些三取代的吡咯并嘧啶核苷由益母霉素制备，并显示出对L1210和P388鼠白血病的抗肿瘤活性。 特定的感兴趣化合物选自以下结构式：其中X是卤素Y是卤素; -NH2; -SH，-SR（其中R是低级烷基，苄基）; -OR（其中OR为甲氧基或烷氧基或其中alk为C1-C6）; 氨基（其中氨基是-NH 2， - 烷基氨基或二烷基氨基，烷基是C 1 -C 6）; γγ二甲基烯丙基氨基; 苄基氨基; 苯基氨基; 硒Z是CN; CXNH 2，其中X是= 0，= S，或= Se，= NH，= NHNH 2，= NOH。 或者Z为= -CH 2 NH 2，-COR = NH Rib =β-D-呋喃核糖基该组化合物的优选成员由以下结构式示出：其中X为Cl Y为Cl或NH 2 Z为CN，CONH 2 ，或C = NOH-NH 2这些化合物进一步鉴定为NSC＃145387（化合物5）NSC＃177369（化合物6）NSC＃182864（化合物8）NSC＃180526（化合物10） 以标准六天方案每隔一天施用13-200mg / kg体重的这些化合物，显示出对L1210和P388鼠白血病的活性（第11号议定书，National Institutes of Health，1972年11月11日） ）。

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