Synthesis and biological evaluation of aryloxazole derivatives as antimitotic and vascular-disrupting agents for cancer therapy

Min Jeong Choi, Eun Sun No, Dhanaji Achyutrao Thorat, Jae Wan Jang, Hakkyun Yang, Jaeick Lee, Hyunah Choo, Soo Jin Kim, Chang Sik Lee, Soo Young Ko, Jiyoun Lee, Ghilsoo Nam, Ae Nim Pae

Research output: Contribution to journalArticlepeer-review

42 Scopus citations

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.

Original languageEnglish
Pages (from-to)9008-9018
Number of pages11
JournalJournal of Medicinal Chemistry
Volume56
Issue number22
DOIs
StatePublished - 27 Nov 2013

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