Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 19, Pages 5565-5568Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.046
Keywords
Thiazolopyridine; Green synthesis; Antioxidant activity; Cytotoxicity
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Funding
- Natural Science Foundation of China [20672090, 200810102050]
- Preliminary Item of Xuzhou Normal University on NSFC [08XLY04]
- Science & Technology Foundation of Xuzhou [XM08C027]
- Qing Lan Project [08QLT001]
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The green chemoselective synthesis of thiazolo[3,2-a]pyridine derivatives was achieved in water via microwave-assisted three-component reactions of malononitrile, aromatic aldehydes and 2-mercaptoacetic acid with molar ratios of 2: 1: 1.5 and 2: 2.2: 1, respectively. These compounds were subject to the experiments of antioxidant activity and cytotoxicity to carcinoma HCT-116 cells and mice lymphocytes. Nearly all of the tested compounds possessed potent capacities for scavenging free radicals. In addition, most of these compounds showed cytotoxicity to HCT-116 cells and mice lymphocytes with no selectivity. Of these, only thiazolo[3,2-a]pyridine derivative 5d suggested selective cytotoxicity to tumor cell line HCT-116 cells. (C) 2009 Elsevier Ltd. All rights reserved.
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