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    • 8. 发明授权
    • DC-89 derivatives
    • DC-89衍生物
    • US5332740A
    • 1994-07-26
    • US46365
    • 1993-04-13
    • Hiromitsu SaitoSatoru NagamuraAkira AsaiEiji KobayashiKatsushige Gomi
    • Hiromitsu SaitoSatoru NagamuraAkira AsaiEiji KobayashiKatsushige Gomi
    • C07D471/04A61K31/435A61K31/495C07D487/04
    • C07D471/04
    • Novel DC-89 derivatives represented by general formula (I): ##STR1## wherein X represents Cl or Br; R.sup.1 represents hydrogen, CONR.sup.2 R.sup.3 (in which R.sup.2 and R.sup.3 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl group), ##STR2## (in which n represents an integer of 4 to 7), ##STR3## (in which R.sup.4 represents oxygen, N--CH.sub.3 or N--CH.sub.2 CH.sub.2 NH.sub.2), ##STR4## (in which R.sup.5 R.sup.6 and R.sup.7 independently represent a straight-chain or branched alkyl group having 1 to 4 carbon atoms); and ##STR5## (in which Y represents hydrogen or CO.sub.2 CH.sub.3); provided that when R.sup.1 is hydrogen, CONR.sup.2 R.sup.3 or SiR.sup.5 R.sup.6 R.sup.7, ##STR6## and pharmaceutically acceptable salts thereof have an excellent anti-tumor activity and are expected to be useful as anti-tumor compositions.
    • 由通式(I)表示的新型DC-89衍生物:其中X表示Cl或Br; R1表示氢,CONR2R3(其中R2和R3独立地表示氢,具有1至4个碳原子的直链或支链烷基或苯基),其中n表示4至7的整数, (其中R 4表示氧,N-CH 3或N-CH 2 CH 2 NH 2),其中R 5和R 7独立地表示碳原子数1〜4的直链或支链烷基。 和其中Y表示氢或CO 2 CH 3)。 条件是当R 1是氢时,CONR 2 R 3或SiR 5 R 6 R 7,其药学上可接受的盐具有优异的抗肿瘤活性,并且预期可用作抗肿瘤组合物。