Synthesis of some new thiazolopyrane and thiazolopyranopyrimidine derivatives bearing a sulfonamide moiety for evaluation as anticancer and radiosensitizing agents

被引：0
作者：
Dalal A. Abou El Ella
Mostafa M. Ghorab
Helmy I. Heiba
Aiten M. Soliman
机构：
[1] Faculty of Pharmacy,Department of Pharmaceutical Chemistry
[2] Ain Shams University,Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC)
[3] College of Pharmacy,Department of Drug Radiation Research
[4] King Saud University,undefined
[5] National Center for Radiation Research and Technology,undefined
来源：
Medicinal Chemistry Research | 2012年 / 21卷
关键词：
Thiazole; Thiazolopyrane; Thiazolopyranopyrimidine; Sulfonamide; Anticancer; Radiosensitizing activities;
D O I：
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中图分类号：
学科分类号：
摘要：
A new series of thiazolopyrane 5a–d, 11–13 and thiazolopyranopyrimidine 6–10, 7b, 8b, and 14 derivatives bearing a sulfonamide moiety were designed and synthesized. The molecular design was performed using molecular operating environment software to predict the binding mode of the proposed compounds on hCAII. All the newly synthesized compounds were evaluated for their in vitro anticancer activity against human liver cancer cell line in which hCAII is overexpressed. Compounds 8b and 14 showed higher activities compared with doxorubicin as a positive control. The radiosensitizing ability of the promising compounds 3, 7a, 8b, 12, and 14 was studied which showed an increase in the cell killing effect of γ-radiation after combination with them.
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页码：2395 / 2407
页数：12
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