Synthesis, antitumor and anti-HIV activities of benzodithiazine-dioxides

被引：27

作者：

Brzozowski, Z

Saczewski, F ^{[1
]}

Neamati, N

机构：

[1] Med Univ Gdansk, Dept Chem Technol Drugs, PL-80416 Gdansk, Poland

[2] Univ So Calif, Sch Pharm, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 09期

关键词：

8-chloro-7-R-1-6-R-2-3-R-3-imidazo[1,2-b][1,4,2]benzodithiazines; synthesis; antitumor activity; anti-HIV activity;

D O I：

10.1016/j.bmc.2005.12.024

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Several 8-chloro-7-R-1-6-R-2-3-R-3-imidazo[1,2-b][1,4,2]benzodithiazine 5,5-dioxide derivatives (9-11, 16-19, and 21-24) have been synthesized as potential antitumor or anti-HIV agents. The in vitro antitumor and anti-HIV-1 activities of the compounds were determined in a panel of cell lines. The benzodithiazine-dioxide 10 showed 50% growth inhibitory activity in low micromolar against most cells. It was particularly effective in leukemia, lung, melanoma, ovarian, and renal cancer cells with GI(50) values of 1-2 mu M. Interestingly, benzodithiazine-dioxide 16 showed remarkable anti-HIV-1 activity with 50% effective concentration EC50 value of 0.94 mu M and no significant cytotoxicity at 200.0 mu M. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：2985 / 2993

页数：9

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