青蒿素-吖啶杂合物的抗肿瘤和抗疟活性。
Antitumour and antimalarial activity of artemisinin-acridine hybrids.
作者信息
Jones Michael, Mercer Amy E, Stocks Paul A, La Pensée Louise J I, Cosstick Rick, Park B Kevin, Kennedy Miriam E, Piantanida Ivo, Ward Stephen A, Davies Jill, Bray Patrick G, Rawe Sarah L, Baird Jonathan, Charidza Tafadzwa, Janneh Omar, O'Neill Paul M
机构信息
Department of Chemistry, University of Liverpool, Crown Street, Liverpool L69 7ZD, UK.
出版信息
Bioorg Med Chem Lett. 2009 Apr 1;19(7):2033-7. doi: 10.1016/j.bmcl.2009.02.028. Epub 2009 Feb 11.
Artemisinin-acridine hybrids were prepared and evaluated for their in vitro activity against tumour cell lines and a chloroquine sensitive strain of Plasmodium falciparum. They showed a 2-4-fold increase in activity against HL60, MDA-MB-231 and MCF-7 cells in comparison with dihydroartemisinin (DHA) and moderate antimalarial activity. Strong evidence that the compounds induce apoptosis in HL60 cells was obtained by flow cytometry, which indicated accumulation of cells in the G1 phase of the cell cycle.
制备了青蒿素-吖啶杂合物，并评估了它们对肿瘤细胞系和恶性疟原虫氯喹敏感株的体外活性。与双氢青蒿素（DHA）相比，它们对HL60、MDA-MB-231和MCF-7细胞的活性提高了2至4倍，并且具有中等抗疟活性。通过流式细胞术获得了这些化合物诱导HL60细胞凋亡的有力证据，这表明细胞在细胞周期的G1期积累。
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