Synthesis and Biological Evaluation of Aryloxazole Derivatives as Antimitotic and Vascular-Disrupting Agents for Cancer Therapy

Title
Synthesis and Biological Evaluation of Aryloxazole Derivatives as Antimitotic and Vascular-Disrupting Agents for Cancer Therapy
Authors
최민정노은선Dhanaji Achyutrao Thorat장재완양학균이재익추현아김수진이창식고수영이지연남길수배애님
Keywords
cancer; tubulin; antimitotic; vascular disrupting agents
Issue Date
2013-11
Publisher
Journal of medicinal chemistry
Citation
VOL 56, NO 22, 9008-9018
Abstract
A series of aryloxazole, thiazole, and isoxazole derivatives was synthesized as vascular-targeting anticancer agents. Antiproliferative activity and tumor vascular-disrupting activity of all of the synthesized compounds were tested in vitro using various human cancer cell lines and HUVECs (human umbilical vein endothelial cells). Several compounds with an arylpiperazinyl oxazole core showed excellent cytotoxicity and metabolic stability in vitro. Among this series, two representative compounds (6-48 and 6-51) were selected and tested for the evaluation of anticancer effects in vivo using tumor-bearing mice. Compound 6-48 effectively reduced tumor growth (42.3% reduction in size) at the dose of 100 mg/kg. We believe that compound 6-48 will serve as a good lead compound for antimitotic and vascular-disrupting agents; further investigation to improve the in vivo efficacy of this series is underway.
URI
http://pubs.kist.re.kr/handle/201004/46833
ISSN
00222623
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KIST Publication > Article
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