Choi, Min Jeong No, Eun Sun Thorat, Dhanaji Achyutrao Jang, Jae Wan Yang, Hakkyun Lee, Jaeick Choo, Hyunah Kim, Soo Jin Lee, Chang Sik Ko, Soo Young Lee, Jiyoun Nam, GhilSoo Pae, Ae Nim 2024-01-20T11:02:51Z 2024-01-20T11:02:51Z 2021-09-05 2013-11-28 0022-2623 https://pubs.kist.re.kr/handle/201004/127422 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. English AMER CHEMICAL SOC TARGETING AGENT COLCHICINE TUBULIN BINDING DISCOVERY INSIGHT DOMAIN SITE Synthesis and Biological Evaluation of Aryloxazole Derivatives as Antimitotic and Vascular-Disrupting Agents for Cancer Therapy Article 10.1021/jm400840p 1 JOURNAL OF MEDICINAL CHEMISTRY, v.56, no.22, pp.9008 - 9018 JOURNAL OF MEDICINAL CHEMISTRY 56 22 9008 9018 scie scopus 000327812600005 2-s2.0-84889263193 Chemistry, Medicinal Pharmacology & Pharmacy Article TARGETING AGENT COLCHICINE TUBULIN BINDING DISCOVERY INSIGHT DOMAIN SITE cancer tubulin antimitotic vascular disrupting agents