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新型7-氯喹啉基硫脲的合成及其作为潜在抗疟和抗癌药物的生物学研究。

Synthesis of new 7-chloroquinolinyl thioureas and their biological investigation as potential antimalarial and anticancer agents.

作者信息

Mahajan Aman, Yeh Susan, Nell Margo, van Rensburg Constance E J, Chibale Kelly

机构信息

Department of Chemistry, University of Cape Town, Private Bag, Rondebosh 7701, South Africa.

出版信息

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5683-5. doi: 10.1016/j.bmcl.2007.07.049. Epub 2007 Aug 19.

DOI:10.1016/j.bmcl.2007.07.049
PMID:17768052
Abstract

New 7-chloroquinolinyl thiourea derivatives derived from the corresponding 4,7-dichloroquinoline isothiocyanate were synthesized and evaluated for in vitro antimalarial and anticancer activity. The most active compound from the series displayed an inhibitory IC(50) value of 1.2 microM against the D10 strain of Plasmodium falciparum. Lack of cytotoxicity towards HeLa cells indicates selectivity towards parasites.

摘要

合成了源自相应的4,7-二氯喹啉异硫氰酸酯的新型7-氯喹啉基硫脲衍生物，并对其体外抗疟和抗癌活性进行了评估。该系列中活性最高的化合物对恶性疟原虫D10株显示出1.2 microM的抑制IC(50)值。对HeLa细胞缺乏细胞毒性表明对寄生虫具有选择性。

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