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本工作研究了一些喜树碱12-取代衍生物的合成,即12-硝基-(Ⅴ),12-氨基-(Ⅵ),12-羟基-(Ⅹ),12-甲氧基-(Ⅺ),12-氰基-(Ⅻ),12-羧基-(ⅩⅢ),12-甲氧羰基-(ⅩⅣ)及12-巯基一喜-树碱(ⅩⅤ)等。取代基的位子是借核磁共振光谱确定的。喜树碱(Ⅰ)在硫酸中硝化得Ⅴ,Ⅴ经催化氢化生成Ⅵ。Ⅵ重氮化后再经适当转换而得到预期的化合物(Ⅶ～ⅩⅤ)。初步药理试验结果表明,Ⅷ对小鼠白血病615有明显抑制作用。Ⅹ及Ⅺ对小鼠艾氏腹水癌的抑制作用强于Ⅰ。进一步的药理试验正在进行中。
This work has investigated the synthesis of some of the camptothecin 12-substituted derivatives, namely 12-nitro- (V), 12-amino- (VI), 12-hydroxy- (XII), 12-cyano- (XII), 12-carboxy- (XIII), 12-methoxycarbonyl- (XIV) and 12-mercapto- The position of the substituent is determined by nuclear magnetic resonance spectroscopy. Camptothecin (Ⅰ) is nitrated in sulfuric acid to form Ⅴ, Ⅴ by catalytic hydrogenation to form Ⅵ. VI diazotization followed by appropriate conversion to give the expected compound (VII ~ XV). Preliminary pharmacological test results show that, Ⅷ on mice leukemia 615 has a significant inhibitory effect. Ⅹ and Ⅺ inhibited Ehrlich ascites carcinoma in mice more than Ⅰ. Further pharmacological tests are underway.