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New diarylureas and diarylamides possessing acet(benz)amidophenyl scaffold: Design, synthesis, and antiproliferative activity against melanoma cell line

Authors
Kim, Hee JinCho, Hye JungKim, HwanEl-Gamal, Mohammed I.Oh, Chang-HyunLee, So HaSim, TaeboHah, Jung-MiYoo, Kyung Ho
Issue Date
May-2012
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Melanoma; Antiproliferative activity; Acet(benz)amidophenyl; Diarylurea; Diarylamide; A375P
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.22, no.9, pp.3269 - 3273
Indexed
SCIE
SCOPUS
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
22
Number
9
Start Page
3269
End Page
3273
URI
https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/33009
DOI
10.1016/j.bmcl.2012.03.020
ISSN
0960-894X
Abstract
A series of new diarylurea and diarylamide derivatives possessing acet(benz)amidophenyl scaffold was synthesized. Their in vitro antiproliferative activity was tested against A375P human melanoma cell line. Compounds 1c,d and 2c,d showed the highest potencies with IC50 values in sub-micromolar scale. In addition, compounds 1b,e,l and 2e,l were more potent than Sorafenib but with IC50 values in micromolar range. Moreover, compound 2c was equipotent to Vemurafenib, and 2d showed higher potency than Vemurafenib against A375P. Molar refractometry calculation and ADME profiling of the highest potent four derivatives 1c,d and 2c,d are also reported. (C) 2012 Elsevier Ltd. All rights reserved.
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