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含1,2,4 - 三嗪部分的杂双环氮体系作为抗艾滋病病毒和抗癌药物的合成，第三部分。

Synthesis of heterobicyclic nitrogen systems bearing the 1,2,4-triazine moiety as anti-HIV and anticancer drugs, part III.

作者信息

el-Gendy Z, Morsy J M, Allimony H A, Ali W R, Abdel-Rahman R M

机构信息

Department of Chemistry, Faculty of Education, Ain Shams University, Roxy, Cairo, Egypt.

出版信息

Pharmazie. 2001 May;56(5):376-83.

PMID:11400552
Abstract

Some new fused heterobicyclic nitrogen systems such as 1,2,4-triazino[3,4-b] [1,3,4] thiadiazolones/thiadiazinones 4-15 and the related compounds 16-21 have been synthesized from treatment of 4-amino-3-mercapto-6-substituted-1,2,4-triazin-5-ones 1 with bifunctional oxygen and halogen compounds via heterocyclization reactions. Structures of the products have been deduced from their elemental analysis and spectral data. Significant anti-HIV and anticancer activities were observed in vitro for some members of the series, compounds 1e, 4e, 4f, 5, 6 and 16 showing a significant activity in Leukemia, Lung, Breast and CNS anticancer evaluation.

摘要

一些新型稠合杂双环氮体系，如1,2,4-三嗪并[3,4-b][1,3,4]噻二唑酮/噻二嗪酮4-15以及相关化合物16-21，是通过4-氨基-3-巯基-6-取代-1,2,4-三嗪-5-酮1与双官能团氧和卤素化合物经杂环化反应合成得到的。产物的结构已通过元素分析和光谱数据推导得出。该系列的一些成员在体外表现出显著的抗HIV和抗癌活性，化合物1e、4e、4f、5、6和16在白血病、肺癌、乳腺癌和中枢神经系统抗癌评估中显示出显著活性。

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