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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
New diarylureas and diarylamides possessing acet(benz)amidophenyl scaffold: Design, synthesis, and antiproliferative activity against melanoma cell line
Bioorganic and Medicinal Chemistry Letters, Volume 22, No. 9, Year 2012
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Description
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 IC 50 values in sub-micromolar scale. In addition, compounds 1b,e,l and 2e,l were more potent than Sorafenib but with IC 50 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. © 2012 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Cho, Hye-jung
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
Oh, Chang-hyun
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
Lee, So-ha
South Korea, Seoul
Korea Institute of Science and Technology
Sim, Taebo
South Korea, Seoul
Korea Institute of Science and Technology
Yoo, Kyung-ho
South Korea, Seoul
Korea Institute of Science and Technology
Statistics
Citations: 34
Authors: 6
Affiliations: 3
Identifiers
Doi:
10.1016/j.bmcl.2012.03.020
ISSN:
14643405