TY - JOUR
T1 - 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives
T2 - A novel type II Raf kinase inhibitors
AU - Yu, Hana
AU - Jung, Yunkyung
AU - Kim, Hwan
AU - Lee, Junghun
AU - Oh, Chang Hyun
AU - Yoo, Kyung Ho
AU - Sim, Taebo
AU - Hah, Jung Mi
N1 - Funding Information:
This research was supported by Korea Institute of Science and Technology and Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology ( 2009-0087992 ; J.M.H.).
PY - 2010
Y1 - 2010
N2 - The synthesis of a novel series of 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives 1a-b, 2a-v and their antiproliferative activities against A375P and WM3629 human melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, pyrazoloimidazole phenyl urea compounds 2a, 2d, 2g, 2i, 2t exhibited potent activities on WM3629 cell lines (IC50 = 0.56-0.86 μM). Especially, 2t was found to be a potent and selective C-Raf inhibitor, showing a possibility as melanoma therapeutics.
AB - The synthesis of a novel series of 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives 1a-b, 2a-v and their antiproliferative activities against A375P and WM3629 human melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, pyrazoloimidazole phenyl urea compounds 2a, 2d, 2g, 2i, 2t exhibited potent activities on WM3629 cell lines (IC50 = 0.56-0.86 μM). Especially, 2t was found to be a potent and selective C-Raf inhibitor, showing a possibility as melanoma therapeutics.
KW - 1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives
KW - Antiproliferative activity
KW - Melanoma cell line
KW - Selectivity
UR - http://www.scopus.com/inward/record.url?scp=77954218062&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2010.04.039
DO - 10.1016/j.bmcl.2010.04.039
M3 - Article
C2 - 20466542
AN - SCOPUS:77954218062
SN - 0960-894X
VL - 20
SP - 3805
EP - 3808
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 12
ER -