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-593
Subject Design, synthesis and antiproliferative activity of N-(2-((4-(3-(3-methoxy and/or hydroxyl)phenyl)-1-phenyl-1H-pyrazol-4-yl)pyridin-2-yl)amino)ethyl) substituted benzene sulfonamides
Authors Mohammed Abdel maksoud, Mohammed EL-Gamal1, Karim Mersal, Usama Ammar, Eslam M. H. Ali, Kyung Ho Yoo2, Chang Hyun Oh3,*
University of Science & Technology, Korea
1Department of Medicinal Chemistry, University of Mansoura, Egypt
2Chemical Kinomics Research Center, Korea Institute of Science and Technology, Korea
3Center for Bio Materials, Korea Institute of Science and Technology, Korea
Abstract Design and synthesis of novel series of N-(2-((4-(3-(3-methoxy and/or hydroxyl)phenyl)-1-phenyl-1H-pyrazol-4-yl)pyridin-2-yl)amino)ethyl) substituted benzene sulfonamides are described. The in vitro antiproliferative activity of the newly synthesized compounds were performed over panel of 60 cell lines belonging to nine different cancer subtypes. KIST 302, KIST 306, KIST 311, KIST 312, KIST 313, KIST 316, KIST 326, KIST328, KIST331, KIST 332, KIST 333, KIST 336 and KIST 337 showed the highest percent inhibition over the 60 cell lines at one dose 10 uM. IC50 for the 13 compounds were determined over each cell line. KIST 332 was the most potent compound over 3 cancer sub types (Leukemia, Colon cancer and Renal Cancer) with IC50 0.42 uM over K-562 cell line, 0.47 uM over HT29 and 0.32 uM over A498 cell line. The most potent compound was tested over 19 different kinases to determine its biological target. In addition normal cell line toxicity and pharmacokinetic were performed for KIST 332.
E-mail ph_ss@hotmail.com