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用于体外抗肿瘤和抗病毒活性的某些嘧啶并[2,1 - b]苯并噻唑和苯并噻唑并[2,3 - b]喹唑啉衍生物的合成。

Synthesis of certain pyrimido[2,1-b]benzothiazole and benzothiazolo[2,3-b]quinazoline derivatives for in vitro antitumor and antiviral activities.

作者信息

el-Sherbeny M A

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

Arzneimittelforschung. 2000 Sep;50(9):848-53. doi: 10.1055/s-0031-1300300.

Abstract

Some new pyrimido[2,1-b]benzothiazole and benzothiazolo[2,3-b]quinazoline derivatives have been synthesized and tested for their antitumor and antiviral activities. Among therm, compounds 5c and 8d exhibited a broad spectrum antitumor activity with full panel (MG-MID) median growth inhibition (GI50) of 11.0 and 11.9 mumol/l, respectively. On the other hand, compounds 5c and 5d showed potential activity against Herpes simplex type-1(HSV-1) with 61 and 50% reduction in the viral plaques, respectively. The detailed synthesis, spectroscopic and biological data are reported.

摘要

已经合成了一些新的嘧啶并[2,1 - b]苯并噻唑和苯并噻唑并[2,3 - b]喹唑啉衍生物,并对其抗肿瘤和抗病毒活性进行了测试。其中,化合物5c和8d表现出广谱抗肿瘤活性,在全组(MG - MID)中的中位生长抑制(GI50)分别为11.0和11.9 μmol/L。另一方面,化合物5c和5d对单纯疱疹病毒1型(HSV - 1)显示出潜在活性,病毒蚀斑分别减少61%和50%。报道了详细的合成、光谱和生物学数据。

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