Welchinskaya H V, Piecuszak B, Kovalenko E A, Sharykina N I, Getman K I, Podgorsky V S
National Medical University, 13 Shevchenko Blvd, Kyiv, 01004, Ukraine.
Mikrobiol Z. 2003 Sep-Oct;65(5):20-5.
A new convenient method for the preparation of heterocyclic bis-adducts: of imidazole, benzimidazole, uracile with 1,1,1-trifluoro-2-bromo-2-chloroethane is described. The reactions are catalysed by the 18-crown-6-complex. The critical toxicity and antitumour activity of saprophytic strains Bacillus genus (B. subtilis 668 IMV and B. polymyxa 102 KSU) extracellular lectins were studies. It was discovered that these substances apply to a few toxic preparations and have a expression antitumour action on the tumours: Walker carcinosarcoma 256, Pliss' lymphosarcoma and Sarcoma 45. The new molecular complexes were created with bacterial lectins and the same heterocyclic-bis-adducts of unsubstituted benzimidazole and 6-methyluracile. A strongly antitumour effect of these complexes has been discovered: of growth relaxation of Pliss' lymphosarcoma tumour mass was 62.5-82.01%.
描述了一种制备咪唑、苯并咪唑、尿嘧啶与1,1,1-三氟-2-溴-2-氯乙烷的杂环双加合物的新简便方法。反应由18-冠-6-配合物催化。研究了腐生芽孢杆菌属（枯草芽孢杆菌668 IMV和多粘芽孢杆菌102 KSU）细胞外凝集素的临界毒性和抗肿瘤活性。发现这些物质适用于几种有毒制剂，并且对肿瘤：沃克癌肉瘤256、普利斯氏淋巴肉瘤和肉瘤45具有明显的抗肿瘤作用。用细菌凝集素与未取代的苯并咪唑和6-甲基尿嘧啶的相同杂环双加合物制备了新的分子复合物。已发现这些复合物具有很强的抗肿瘤作用：普利斯氏淋巴肉瘤肿瘤块的生长缓解率为62.5-82.01%。
