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銻胺羧螯合物是本所发現的新型抗肿瘤药物,本文继續探討此类化合物的化学結构与疗效之間关系。发現:(1)銻与5种不同类型的胺羧螯合剂結合的制剂,例如EDTA-Sb(Ⅰ)和PDTA-Sb(Ⅳ)的不同盐类,N取代的EDTA-Sb(Ⅱ),ATA-Sb(Ⅴa)及其类似物(Ⅶ)和GDTA-Sb(Ⅸf)对小鼠Ehrlich腹水瘤均有明显的抑制作用,其中乙二胺四乙酸銻丙基銨盐和对氧氮六环盐的疗效較其鈉盐为佳。(2)汞、鉍、鉛、鋅、錳、銅、鈷、鎳、錫和鋇10种金属胺羧絡合物(Ⅲ,Ⅴ及Ⅷ)及EDTA,PDTA和ATA对Ehrlich腹水瘤和肉瘤180均无疗效。(3)EDTA-Sb-Na,PDTA-Sb-Na和ATA-Sb对肉瘤180稍有抑制作用。(4)銻胺羧螯合物抗癌作用的基本結构可能为一个含銻的螯合物分子中拥有以氮为中心而具有三个以上的羧甲基。
Antimony amines carboxylate chelates discovered by the new antitumor drugs, the paper continued to explore the chemical structure of such compounds and the relationship between curative effect. It has been found that: (1) different antimony binding agents with 5 different types of amine carboxy-chelating agents such as different salts of EDTA-Sb (I) and PDTA-Sb ATA-Sb (Va) and its analogs (Ⅶ) and GDTA-Sb (Ⅸf) have obvious inhibitory effects on mouse Ehrlich ascites tumor, in which antimony ammonium salt of ethylenediaminetetraacetic acid and p- The efficacy of salt is better than its sodium salt. (2) Ehrlich ascites tumor and sarcoma 180 with EDTA, PDTA and ATA, 10 kinds of metal amine amine complexes (Ⅲ, Ⅴ and Ⅷ) of Mercury, Bismuth, Lead, Zinc, Manganese, Copper, Cobalt, Nickel, No effect. (3) EDTA-Sb-Na, PDTA-Sb-Na and ATA-Sb slightly inhibit sarcoma 180. (4) The basic structure of anticancer amine carboxylate chelate anticancer effect may be that an antimony-containing chelate molecule has more than three carboxymethyl groups centered on nitrogen.