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缩氨基硫脲类是近年来国外在筛选过程中发现的具有较好疗效和较新结构的抗癌药物。其中以 5-羟基嘧啶-2-甲醛缩氨基硫脲(5-HP)为最好,已进入白血病治疗的临床试验阶段,其作用机制是与体内的铁离子螯合而抑制核糖核酸还原酶从而阻断了 DNA 的合成。该类药物的今后动向值得注意,为此我们于1973年合成了5-HP 并且由浙江卫生实验院进行药理试验。早在1956年,Brockman 就发现嘧啶-2-甲醛缩氨基硫脲(Ⅰ)有一定的抗白血病作用,但因累积性毒性太大而不能应用。随后,F.A.French 研究了许多易得的芳香醛和杂
The thiosemicarbazones are anticancer drugs with good efficacy and relatively new structure found in the screening process abroad. Among them, 5-hydroxypyrimidine-2-carboxaldehyde thiosemicarbazone (5-HP) is the best and has entered the clinical trial stage of leukemia treatment. Its mechanism of action is to chelate iron ions in the body and inhibit ribonucleotide reductase. Blocked DNA synthesis. The future trends of this class of drugs are worth noting. For this reason, we synthesized 5-HP in 1973 and conducted pharmacological tests by the Zhejiang Hygiene Laboratory. As early as 1956, Brockman found that pyrimidine-2-carboxaldehyde thiosemicarbazone (I) had some anti-leukemia effect, but could not be used due to too large cumulative toxicity. Subsequently, F.A. French studied many available aromatic aldehydes and impurities.