本文报道标题化合物的合成及其抗疟、抗肿瘤和抗菌活性,该类化合物是以5-氯-2,4, 6-三氨基喹唑啉与各种取代苯甲醛缩合成相应的Schiff碱,然后经NaBH_4还原,再甲酰化或亚硝化制得.经对感染伯氏疟原虫(P.berghei)的鼠抑制性治疗筛选,有八...本文报道标题化合物的合成及其抗疟、抗肿瘤和抗菌活性,该类化合物是以5-氯-2,4, 6-三氨基喹唑啉与各种取代苯甲醛缩合成相应的Schiff碱,然后经NaBH_4还原,再甲酰化或亚硝化制得.经对感染伯氏疟原虫(P.berghei)的鼠抑制性治疗筛选,有八个化合物剂量20mg/kg×4d时抑制率100%,Ⅰ_3,Ⅰ_4,Ⅲ_4三个化合物剂量5mg/kg×4d时抑制率在90%以上;体外抗肿瘤试验有4个化合物的活性优于MTX和SIPl759,以Ⅰ_4最佳。对L1210白血病细胞株的IC_(50)为2.20×10^(-9) m mol/L;经对18种常用菌株进行体外筛选,发现对肺炎双球菌(D.pneumoniae)有较好的活性。展开更多
AIM To search for antineoplastic drugs with fewer side effects and improved activities, using tetrazine derivatives with different substituted groups in their phenyl rings. METHODS The title compounds have been synthe...AIM To search for antineoplastic drugs with fewer side effects and improved activities, using tetrazine derivatives with different substituted groups in their phenyl rings. METHODS The title compounds have been synthesized by reacting 3,6-dimethyl-1,6-dihydro-1,2,4,5-tetrazine with substituted phenyl isocyanates in the precence of p-dimethylamino pyridine as catalyst. RESULTS Eighteen new N,N ′-disubstituted phenyl-3,6-dimethyl-1,4-dihydro-1,2,4,5-tetrazine-1,4-dicarboamides have been synthesized. Their structures have been comfirmed by IR, 1HNMR and elemental analysis. The antineoplastic activities were screened. The structure-activity relationship has also been studied. CONCLUSION The meta-substituted tetrazine derivatives showed marked antitumor activities against P388 and A-549 when electronic effect constants and hydrophobic constants of their substitutents are in a certain range.展开更多
文摘本文报道标题化合物的合成及其抗疟、抗肿瘤和抗菌活性,该类化合物是以5-氯-2,4, 6-三氨基喹唑啉与各种取代苯甲醛缩合成相应的Schiff碱,然后经NaBH_4还原,再甲酰化或亚硝化制得.经对感染伯氏疟原虫(P.berghei)的鼠抑制性治疗筛选,有八个化合物剂量20mg/kg×4d时抑制率100%,Ⅰ_3,Ⅰ_4,Ⅲ_4三个化合物剂量5mg/kg×4d时抑制率在90%以上;体外抗肿瘤试验有4个化合物的活性优于MTX和SIPl759,以Ⅰ_4最佳。对L1210白血病细胞株的IC_(50)为2.20×10^(-9) m mol/L;经对18种常用菌株进行体外筛选,发现对肺炎双球菌(D.pneumoniae)有较好的活性。
文摘AIM To search for antineoplastic drugs with fewer side effects and improved activities, using tetrazine derivatives with different substituted groups in their phenyl rings. METHODS The title compounds have been synthesized by reacting 3,6-dimethyl-1,6-dihydro-1,2,4,5-tetrazine with substituted phenyl isocyanates in the precence of p-dimethylamino pyridine as catalyst. RESULTS Eighteen new N,N ′-disubstituted phenyl-3,6-dimethyl-1,4-dihydro-1,2,4,5-tetrazine-1,4-dicarboamides have been synthesized. Their structures have been comfirmed by IR, 1HNMR and elemental analysis. The antineoplastic activities were screened. The structure-activity relationship has also been studied. CONCLUSION The meta-substituted tetrazine derivatives showed marked antitumor activities against P388 and A-549 when electronic effect constants and hydrophobic constants of their substitutents are in a certain range.
