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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines
European Journal of Medicinal Chemistry, Volume 46, No. 8, Year 2011
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Description
Synthesis of a new series of diarylureas and diarylamides having 1H-pyrrolo[3,2-c]pyridine scaffold is described. Their in vitro antiproliferative activity against A375P human melanoma cell line was tested and the effect of substituents on pyrrolo[3,2-c]pyridine nucleus was investigated. The newly synthesized compounds, except three N-tolyl derivatives (8f, 9f, and 9h), generally showed superior activity against A375P to Sorafenib. Among all of these derivatives, compounds 8b, 8g, and 9a-e showed the highest potency against A375P with IC50 in nanomolar range. In addition, compounds 8d, 8e, 8h, 9g, 9i, and 9j were more potent than Sorafenib but with IC 50 in micromolar range. Compounds 8b, 8g, 9b-d, and 9i demonstrated higher selectivity towards A375P compared with NIH3T3 fibroblasts. The most potent diarylurea 8g and diarylamide 9d were further tested and showed high potency over nine melanoma cell lines at the NCI. © 2011 Elsevier Masson SAS. All rights reserved.
Authors & Co-Authors
El-Gamal, Mohammed I.
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
Jung, Myung-ho
South Korea, Seoul
Korea Institute of Science and Technology
Lee, Woongsan
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
Oh, Chang-hyun
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
Statistics
Citations: 32
Authors: 6
Affiliations: 2
Identifiers
Doi:
10.1016/j.ejmech.2011.04.031
ISSN:
17683254