Synthesis, structure and hypoxic cytotoxicity of 3-amino-1,2,4-benzotriazine-1,4-dioxide derivatives
Synthesis, structure and hypoxic cytotoxicity of 3-amino-1,2,4-benzotriazine-1,4-dioxide derivatives
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DOI：
10.1002/ardp.200600201
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发表时间：
2007-05-01
影响因子：
5.1
通讯作者：
Hu, Yongzhou
中科院分区：
文献类型：
--
作者：
Jiang, Faqin;Weng, Qinjie;Hu, Yongzhou
合成了一系列新的3-氨基-1，2，4-苯并三嗪-1，4-二氧化物衍生物，并对其在缺氧和常氧条件下对早幼粒细胞白血病HL-60、雄激素非依赖性前列腺癌PC-3、肝癌Bel-7402、人食管癌ECA-109和人乳腺癌MCF-7细胞系的体外细胞毒性进行了筛选。大多数化合物在缺氧和常氧条件下均表现出较高的细胞毒活性。其中，与替拉扎明相比，化合物61和62显示出更强的细胞毒活性和缺氧选择性。
A series of novel 3-amino-1,2,4-benzotriazine-1,4-dioxide derivatives were synthesized and screened for their in vitro cytotoxicity against promyelocytic leukemia HL-60, androgen-independent prostate tumor PC3, hepatocellular carcinoma Bel-7402, human esophagus tumor ECA-109, and human breast tumor MCF-7 cell lines in hypoxia and in normoxia. Most compounds showed higher cytotoxic activity both in hypoxia and in normoxia. Among them, compounds 61 and 62 showed more potent cytotoxic activity and hypoxic selectivity when compared to tirapazamine.