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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and biological activity of new 2-amino-8-chloro-5,5-dioxo(1,2,4)triazolo(2,3-b)(1,4,2)benzodithiazines.
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Synthesis and biological activity of new 2-amino-8-chloro-5,5-dioxo(1,2,4)triazolo(2,3-b)(1,4,2)benzodithiazines.

机译：新型2-氨基-8-氯-5,5-二氧杂（1,2,4）三唑（2,3-b）（1,4,2）苯并二噻嗪的合成及生物活性。

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摘要

Two series of 1-(6-chloro-1,1-dioxo-1,4,2-benzodithiazin-3-yl)-4-arylsemicarbazides 6-17 and 2-arylamino-8-chloro-5,5-dioxo[1,2,4]triazolo[2,3-b][1,4,2]benzodithiazine s 18-26 were prepared in order to evaluate their biological activity. Compounds 6 and 18-26 were tested for their in vitro cytotoxic potency against 12 human cancer cell lines. The compounds 6 and 19 were inactive, whereas triazolobenzodithiazines 18, 20-26 possess tumor growth inhibitory properties. The prominent methyl 8-chloro-2-(4-chlorophenylamino)-5,5-dioxo[1,2,4]triazolo[2,3-b][1,4,2]ben zodithiazine-7-carboxylate (21) exhibited potency higher or comparable to cisplatin. Moreover, compounds 6, 9, 19 and 23-25 with structure similar to other chemotherapeutic agents were tested for their antibacterial activity and exhibited MIC and MBC against Staphylococcus aureus (3.9-31.5 microg ml).
机译：1-（6-氯-1,1-二氧代-1,4,2-苯并噻唑嗪-3-基）-4-芳基氨基脲的两个系列6-2-17和2-芳基氨基-8-氯-5,5-二氧杂[制备1,2,4]三唑并[2,3-b] [1,4,2]苯并二噻嗪s 18-26以评估其生物学活性。测试化合物6和18-26对12种人类癌细胞系的体外细胞毒性效力。化合物6和19是无活性的，而三唑并苯并二噻嗪18、20-26具有抑制肿瘤生长的特性。著名的8-氯-2-（4-氯苯基氨基）-5,5-二氧杂[1,2,4]三唑[2,3-b] [1,4,2]苯并噻嗪-7-羧酸甲酯（21 ）表现出更高的效力或可与顺铂媲美。此外，测试了具有与其他化学治疗剂相似结构的化合物6、9、19和23-25的抗菌活性，并显示出针对金黄色葡萄球菌的MIC和MBC（3.9-31.5微克/毫升）。

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