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DERIVATIVES OF XANTHINE WITH ANTI-PROLIFERATING ACTIVITY, MODULATORS OF CELLULAR DIFFERENTIATION

机译:黄嘌呤具有抗增殖活性的衍生物,细胞分化的调节剂

摘要

1. xanthine derivatives or pharmaceutically acceptable derivatives of formula 1! ! where! R1 is CH3, R2 - CH3; R3 - halogens F, Cl, Br, I; R4 - hydrogen; ! R1 is CH3, R2 - CH3; R3 - hydrogen, halogens F, Cl, Br, I; R4-CH2COOH; ! R1 is hydrogen, R2 - CH3; R3 - halogens F, Cl, Br, I; R4 - CH3. ! 2. A compound according to claim 1, wherein R1, R2 and R4 each independently is CH3, a R3 - hydrogen: 1,3,7, -trimetilksantin (caffeine). ! 3. A compound according to claim 1, wherein R1 and R3 each is independently hydrogen, a R2 and R4 each independently of the other is CH3: 3.7, -dimetilksantin (theobromine). ! 4. A compound according to claim 1, wherein R1 and R2 represent each independently CH3, a R3 and R4 each independently represents H: 1.3, -dimetilksantin (theophylline). ! 5. A compound according to claim 1, wherein R1 and R2 represent each independently CH3, a R3 is Cl and R4 is H: 8-chloro-1,3, -dimetilksantin (8-hlorteofillin). ! 6. A compound according to claim 1, wherein R1 and R2 represent each independently CH3, a R3 is Br and R4 is H: 8-bromo-1,3, -dimetilksantin (8-bromo-theophylline). ! 7. A compound according to claim 1, wherein R1 and R2 represent each independently CH3, a R3 is H and R4 is CH2COOH: 1.3 -dimetilksantin-7-acetate (theophylline-7-acetate). ! 8. A method of slowing the rate of proliferation of tumor cells, comprising administering to the environment an acceptable amount of an active compound, characterized in that as active compound a compound administered according to any of claims 1-7. ! 9. A method according to claim 8, characterized in that said compound is administered in an amount of 1 mM. ! 10. The process of differentiation induction in cells of mouse melanoma B16-F10, comprising administering to the environment an acceptable amount of active
机译:1.式1的黄嘌呤衍生物或可药用衍生物! !哪里! R1是CH3,R2-CH3; R3-卤素F,Cl,Br,I; R 4-氢; ! R1是CH3,R2-CH3; R 3-氢,卤素F,Cl,Br,I; R4-CH2COOH; ! R1是氢,R2-CH3; R3-卤素F,Cl,Br,I; R4-CH3。 ! 2.根据权利要求1的化合物,其中R1,R2和R4各自独立地是CH3,R3-氢:1,3,7,-三甲必西汀(咖啡因)。 ! 3.根据权利要求1的化合物,其中R1和R3各自独立地是氢,R2和R4彼此独立地是CH3:3.7,-二美替沙坦(可可碱)。 ! 4.根据权利要求1的化合物,其中R1和R2各自独立地代表CH3,R3和R4各自独立地代表H:1.3,-二枯草黄素(茶碱)。 ! 5.根据权利要求1所述的化合物,其中R1和R2各自独立地代表CH3,R3是Cl,并且R4是H:8-氯-1,3,-二美替西坦(8-芦丁菲金)。 ! 6.根据权利要求1的化合物,其中R1和R2各自独立地代表CH3,R3是Br,R4是H:8-溴-1,3,-二美替西坦(8-溴-茶碱)。 ! 7.根据权利要求1的化合物,其中R1和R2各自独立地代表CH3,R3是H,并且R4是CH2COOH:1.3-二枯​​基西汀-7-乙酸盐(茶碱-7-乙酸盐)。 ! 8.一种减慢肿瘤细胞增殖速率的方法,包括向环境施用可接受量的活性化合物,其特征在于,根据权利要求1-7中任一项施用的化合物作为活性化合物。 ! 9.根据权利要求8的方法,其特征在于所述化合物以1mM的量给药。 ! 10.在小鼠黑素瘤B16-F10的细胞中诱导分化的方法,包括向环境施用可接受量的活性剂。

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