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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
New diarylureas and diarylamides containing 1,3,4-triarylpyrazole scaffold: Synthesis, antiproliferative evaluation against melanoma cell lines, ERK kinase inhibition, and molecular docking studies
European Journal of Medicinal Chemistry, Volume 46, No. 12, Year 2011
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Description
Synthesis of a new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold is described. Their in vitro antiproliferative activities against 9 human melanoma cell lines were tested. Compounds 12, 13, 15, and 21-23 showed the highest potency against A375P melanoma cell line. In addition, compounds 10-15 and 19-24 showed high potency over the NCI 8 tested melanoma cell-lines panel. The IC50 values for compound 23 were 0.36 μM and 0.84 μM over LOX IMVI and M14 cell lines, respectively. Compounds 21 and 23 showed high, dose-dependent inhibition of ERK kinase. Virtual screening was carried out through docking of compound 21 into the domain of V600E-B-RAF and the binding mode was studied. © 2011 Elsevier Masson SAS. All rights reserved.
Authors & Co-Authors
Choi, Won-kyoung
South Korea, Seoul
Korea Institute of Science and Technology
El-Gamal, Mohammed I.
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
Choi, Hongseok
South Korea, Gwangju
Chosun University
Baek, Daejin
South Korea, Seosan
Hanseo University
Oh, Chang-hyun
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
Statistics
Citations: 72
Authors: 5
Affiliations: 4
Identifiers
Doi:
10.1016/j.ejmech.2011.08.013
ISSN:
17683254