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Methyl berberrubin and palmatrubin esters - inhibitors of growth of transplanted sarcomas
Methyl berberrubin and palmatrubin esters - inhibitors of growth of transplanted sarcomas
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机译:甲基小ber红素和棕榈红素酯-移植肉瘤的生长抑制剂
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摘要
13-Methyl berbine derivs. of formula (I) are new: R1 and R2 are each CH3O or together form methylenedioxy; R3 = CH3, 4-methoxyphenyl or phenylvinyl; and X = pharmaceutically tolerable anion. They are prepd. by conventional acylation of 13-methylberberrubin or 13-methylpalmatrubin. (I) inhibit the growth of transplanted sarcoma in mice. E. g where X = Cl the cpds. gave 100% inhibition of sarcoma S180 when given at 30 mg/kg/day for 5 consecutive days. Specif (I) e.g. 13-methylberberrubin acetate chloride (1.8g) was prepd. by reacting 3g 13-methylberberrubin with 1.2g acetyl chloride in CHCl3-pyridine.
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机译:13-甲基贝宾碱衍生物。式(I)的化学式是新的:R 1和R 2各自为CH 3 O或一起形成亚甲基二氧基; R3 = CH3、4-甲氧基苯基或苯基乙烯基; X =药学上可接受的阴离子。他们准备好了。通过常规的酰化13-甲基小ber红素或13-甲基palmatrubin。 (I)抑制小鼠移植肉瘤的生长。例如,其中X = Cl cpds。连续5天以30 mg / kg /天的剂量给予肉瘤S180抑制100%。规格(I)例如制备13-甲基小rub红素乙酸盐氯化物(1.8g)。使3g 13-甲基小ber红素与1.2g乙酰氯在CHCl3-吡啶中反应
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