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镓(III)与7-氯喹啉硫代半卡巴腙形成的配合物作为配体具有高效的抗增殖作用:合成、细胞毒性及抗疟活性评价

Highly potent anti-proliferative effects of a gallium(III) complex with 7-chloroquinoline thiosemicarbazone as a ligand: synthesis, cytotoxic and antimalarial evaluation.

作者信息

Kumar Kewal, Schniper Sarah, González-Sarrías Antonio, Holder Alvin A, Sanders Natalie, Sullivan David, Jarrett William L, Davis Krystyn, Bai Fengwei, Seeram Navindra P, Kumar Vipan

机构信息

Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.

Department of Chemistry and Biochemistry, The University of Southern Mississippi, 118 College Drive, # 5043, Hattiesburg, MS 39406-0001, USA.

出版信息

Eur J Med Chem. 2014 Oct 30;86:81-6. doi: 10.1016/j.ejmech.2014.08.054. Epub 2014 Aug 16.

Abstract

A gallium(III) complex with 7-chloroquinoline thiosemicarbazone was synthesized and characterized. The complex proved to be thirty-one times more potent on colon cancer cell line, HCT-116, with considerably less cytotoxicity on non-cancerous colon fibroblast, CCD-18Co, when compared to etoposide. Its anti-malarial potential on 3D7 isolate of Plasmodium falciparum was better than lumefantrine.

摘要

合成并表征了一种含有7-氯喹啉硫代半卡巴腙的镓(III)配合物。与依托泊苷相比,该配合物对结肠癌细胞系HCT-116的活性高31倍,而对非癌性结肠成纤维细胞CCD-18Co的细胞毒性则小得多。其对恶性疟原虫3D7分离株的抗疟潜力优于卤泛群。

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