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由5(及7)-[双-(β-羥乙基)-氨基]吲(口朶)-2-羧酸乙酯(Ⅶ_(a,b))合成了5(及7)-[双-(β-氯乙基)-氨基]吲(口朶)-2-羧酸乙酯(Ⅱ_a和Ⅱ_b)、5(及7)-[双-(β-溴乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅱ_c和Ⅱ_d)以及5(及7)-[双-(β-碘乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅱ_e和Ⅱ_f)。再經水解制得其相应的羧酸(I_(a-f))。此外又合成了5(及7)-乙氧羰氨基-吲(口朶)-2-羧酸乙酯(IX_(a,b))和5-乙氧基-7-[双-(β-氯乙基)-氨基]-吲(口朶)-2-羧酸乙酯(Ⅶ)。化合物I_a,I_b,I_c,Ⅱ_a,Ⅱ_b,Ⅱ_c,Ⅱ_e和Ⅱ_f对組織培养Hela細胞有明显的抑制作用。化合物Ⅰ_a,Ⅰ_b,Ⅱ_a和Ⅱ_b口服时对小鼠肉瘤180有明显的抑制作用。化合物Ⅰ_e,Ⅰ_f和Ⅻ对肉瘤180具有中度的抑制作用。
Synthesis of 5 (and 7) - [bis (4-hydroxyethyl) amino] indole (Ⅱa and Ⅱ_b), 5 (and 7) - [bis- (β-bromoethyl) -amino] -indole (Oral) -2-carboxylic acid ethyl ester (Ⅱ_c and Ⅱ_d) and 5 (and 7) - [bis- (β-iodoethyl) -amino] Ⅱ_e and Ⅱ_f). Then by hydrolysis to the corresponding carboxylic acid (I_ (a-f)). In addition, 5 (and 7) -ethoxycarbonylamino-indole-2-carboxylic acid ethyl ester (IX_ (a, b)) and 5-ethoxy-7- [bis- Chloroethyl) -amino] -indole (Oral) -2-carboxylic acid ethyl ester (VII). Compound I_a, I_b, I_c, Ⅱ_a, Ⅱ_b, Ⅱ_c, Ⅱ_e and Ⅱ_f on Hela cells were significantly inhibited. Compound Ⅰ_a, Ⅰ_b, Ⅱ_a and Ⅱ_b oral administration of sarcoma 180 mice had a significant inhibitory effect. Compounds Ⅰ_e, Ⅰ_f and Ⅻ have a moderate inhibitory effect on sarcoma 180.