青蒿素衍生的、化学性质稳定的三氧杂环乙烷二聚体的抗疟、抗增殖和抗肿瘤活性。

Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers.

作者信息

Posner G H, Ploypradith P, Parker M H, O'Dowd H, Woo S H, Northrop J, Krasavin M, Dolan P, Kensler T W, Xie S, Shapiro T A

机构信息

Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, Maryland 21218, USA.

出版信息

J Med Chem. 1999 Oct 21;42(21):4275-80. doi: 10.1021/jm990363d.

DOI:10.1021/jm990363d

PMID:10543871

Abstract

Nine C-10 non-acetal derivatives of the natural trioxane artemisinin (1) were prepared as dimers using some novel chemistry. As designed, each dimer was stable chemically. C-10 Olefinic dimers 7 and C-10 saturated dimers 8-13 all showed good to excellent antimalarial and antiproliferative activities in vitro. Dimers 8, 10, and 12 were especially potent and selective at inhibiting growth of some human cancer cell lines in the NCI in vitro 60-cell line assay.

摘要

利用一些新颖的化学方法，制备了天然三氧杂环已烷青蒿素（1）的9种C-10非缩醛衍生物作为二聚体。如设计的那样，每个二聚体在化学上是稳定的。C-10烯烃二聚体7和C-10饱和二聚体8 - 13在体外均表现出良好至优异的抗疟和抗增殖活性。在国立癌症研究所（NCI）的体外60细胞系试验中，二聚体8、10和12在抑制某些人类癌细胞系生长方面特别有效且具有选择性。