Antineoplastic and Cytotoxic Activities of Nickel(II) Complexes of Thiosemicarbazones.
Antineoplastic and Cytotoxic Activities of Nickel(II) Complexes of Thiosemicarbazones.
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DOI：
10.1155/mbd.1997.89
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发表时间：
1997-01-01
期刊：
影响因子：
--
通讯作者：
West, D X
中科院分区：
文献类型：
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作者：
Hall, I H;Miller, M C;West, D X
缩氨基硫脲的镍(II)络合物对人和啮齿动物组织培养的肿瘤细胞具有很强的细胞毒作用。每种化合物在不同组织学类型的肿瘤中表现出略有不同的特征。APIP的镍络合物在艾氏腹水癌中显示出最强的体内活性。该药选择性地抑制L1210DNA和嘌呤的合成，以及DNA聚合酶α、PRPP-氨基转移酶、IMP-脱氢酶、二氢叶酸还原酶、TMP-激酶和胸苷合成酶的活性。孵育24小时后，L1210细胞DNA断裂明显，DNA粘度降低。镍配合物不是L1210 DNA拓扑异构酶II抑制剂。
Nickel(II) complexes of thiosemicarbazons were observed to be potent cytotoxic agents in human and rodent tissue cultured tumor cells. Each compound demonstrated a slightly different profile in the various histological types of tumors. The nickel complex of Appip demonstrated the most potent in vivo activity in the Ehrlich ascites carcinoma. This agent selectively inhibited L1210 DNA and purine syntheses, and DNA polymerase alpha, PRPP-amido transferase, IMP-dehydrogenase, dihydrofolate reductase, TMP-kinase and thymidylate synthetase activities. L1210 DNA strand scission was evident and DNA viscosity was reduced after 24 hr incubation. The nickel complexes were not L1210 DNA topoisomerase II inhibitors.