121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-594
Subject Anticancer activity of newly synthesized imidazo[2,1-b]oxazole derivatives as V600E BRAF inhibitors for treatment of melanoma
Authors Mohammed Abdel maksoud, Mohammed EL-Gamal1, Usama Ammar2, Eslam M. H. Ali2, Karim Mersal2, Kyung Ho Yoo3, Chang Hyun Oh4,*
University of Science & Technology, Egypt
1Department of Medicinal Chemistry, University of Mansoura, Egypt
2Center for Bio Materials, University of Science & Technology, Egypt
3Chemical Kinomics Research Center, Korea Institute of Science and Technology, Korea
4Center for Bio Materials, Korea Institute of Science and Technology, Korea
Abstract The aim of current study is to synthesis a new series of imidazo[2,1-b]oxazole with different substitutions at position 5 and 6. The in vitro antiproliferative activity of the novel compounds were tested against melanoma cell line. KIST 211, KIST 212, KIST 215, KIST 216, KIST 226, KIST 231, KIST 235, KIST 236 and KIST 242 showed high activity against A375 cell line. The most potent compounds were tested for their activity over CRAF, BRAF, V600E BRAF and P38 alpha. The ten compounds exhibited activity ranging from 90-100% against the 4 enzymes at 10 μM. Compounds containing m-OH phenyl at position 6 and 2-substituted pyrimidine at position 5 with propyl bridge between pyrimidine and sulfonamide moiety showed the highest activity.
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