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硫杂脯氨酸是一种新型抗癌药。为降低其毒性,我们合成了五种硫杂脯氨酸糖衍生物:1—0—(N—乙酰—L—TCA)—2,3,4,6—四—0—乙酰—β—D—葡萄糖(Ⅳ_a);1—0—(N—乙酰—dL—TCA)—2,3,4,6—四—0—乙酰—β—D—葡萄糖(Ⅳ_b);1—0—(N—乙酰—dL—TCA)—2,3,4—三—0—乙酰—β—D—葡萄糖醛酸甲酯(Ⅴ);1,5—二—0—(N—Z—酰—L—TCA)—葡萄糖醛酸γ内酯(Ⅵ_a),和1,5—二—0—(N—乙酰—dL—TCA)—萄萄糖醛酸γ内酯((Ⅵ_b),以期在体内糖苷酶和酯酶的作用下,缓慢将TCA释出,达到降低毒性的目的。上列化合物均未见报导,其结构均被红外光谱、核磁共振谱、质谱和元素分析等结果所证实。化合物(Ⅵ_b)的初步抑瘤试验表明,其对小鼠S_(180)肉瘤的抑瘤率为36.9％。其它化合物待测。
Thiol proline is a new anticancer drug. To reduce their toxicity, we synthesized five thiaproline sugar derivatives: 1-0- (N-acetyl-L-TCA) -2,3,4,6-tetra-O-acetyl-β-D 1-N- (N-acetyl-dL-TCA) -2,3,4,6-tetra-O-acetyl-β-D-glucose Acetyl-dL-TCA) -2,3,4-tri-O-acetyl-β-D-glucuronate; ) -galactono-γ-lactone (Ⅵ_a) and 1,5-di-O- (N-acetyl-dL-TCA) -glucuronolactone (Ⅵ_b) Esterase, the TCA was released slowly to achieve the purpose of reducing the toxicity.The above compounds have not been reported, the structures of which are confirmed by the results of infrared spectrum, nuclear magnetic resonance spectrum, mass spectrum and elemental analysis, etc. Compound (VI_b) The preliminary antitumor test showed that the antitumor activity of the antitumor agent on mouse S_ (180) sarcoma was 36.9%, and other compounds were tested.