New Diarylureas and Diarylamides Possessing Acet(benz)amidophenyl Scaffold: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line

Title
New Diarylureas and Diarylamides Possessing Acet(benz)amidophenyl Scaffold: Design, Synthesis, and Antiproliferative Activity against Melanoma Cell Line
Authors
김희진조혜정김환엘가말오창현이소하심태보하정미유경호
Keywords
Melanoma; Antiproliferative activity; Acet(benz)amidophenyl; Diarylurea; Diarylamide; A375P
Issue Date
2012-05
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 22, NO 9, 3269-3273
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.
URI
http://pubs.kist.re.kr/handle/201004/42431
ISSN
0960894X
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KIST Publication > Article
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