Synthesis and in vitro antitumor activity of new series of benzothiazole and pyrimido[2,1-b]benzothiazole derivatives

被引：58
|
作者：
Gabr, Moustafa T. [1 ]
El-Gohary, Nadia S. [1 ]
El-Bendary, Eman R. [1 ]
El-Kerdawy, Mohamed M. [1 ]
机构：
[1] Mansoura Univ, Dept Med Chem, Fac Pharm, Mansoura 35516, Egypt
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 85卷
关键词：
Benzothiazoles; Pyrimidobenzothiazoles; Synthesis; Antitumor activity; Pharmacophore study; NATIONAL-CANCER-INSTITUTE; BIOLOGICAL EVALUATION; 3-D PHARMACOPHORES; AURORA INHIBITORS; POTENTIAL AGENTS; DRUG DISCOVERY; LUNG; MOIETY; ERLOTINIB; SEARCH;
D O I：
10.1016/j.ejmech.2014.07.097
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
New series of benzothiazole and pyrimido[2,1-b]benzothiazole derivatives were synthesized and characterized by analytical and spectrometrical methods (IR, HRMS, H-1 and C-13 NMR). Nineteen of the synthesized compounds were selected by the National Cancer Institute (NCI), USA, to be screened for their antitumor activity at a single dose (10 mu M) against a panel of 60 cancer cell lines. The most active compounds, 4, 6, 10, 14, 17 and 20 were selected for further evaluation at five dose level screening. Compounds 17 (GI(50) = 0.44 mu M, TGI = 1.2 mu M and LC50 MG-MID = 6.6 mu M) and 4 (GI(50) = 0.77 mu M, TGI = 2.08 mu M and LC50 MG-MID = 11.74 mu M) were proved to be the most active members in this study. 3D and 2D pharmacophoric maps for the structural features of both compounds were studied. (C) 2014 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：576 / 592
页数：17
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