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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Design, synthesis, and antiproliferative activity of new 1H-pyrrolo[3,2-c]pyridine derivatives against melanoma cell lines. Part 2
Bioorganic and Medicinal Chemistry Letters, Volume 22, No. 13, Year 2012
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Description
A new series of diarylureas and diarylamides possessing 1H-pyrrolo[3,2-c]pyridine scaffold was designed and synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-9 human melanoma cell line panel were tested. All the target compounds, except three amino derivatives 8g, h and 9h, demonstrated superior potencies against A375P to Sorafenib. In addition, compounds 8a and 9b-f demonstrated higher potencies than Vemurafenib against A375P. Compounds 8c and 9b were 7.50 and 454.90 times, respectively, more selective towards A375P melanoma cells over NIH3T3 fibroblasts. Furthermore, compounds 8d, e and 9a-d, f demonstrated very high potencies against the nine tested melanoma cell lines at the NCI. The bisamide derivatives 9a-c, f showed 2-digit nanomolar IC 50 values over different cell lines of the NCI-9 melanoma cell lines. © 2012 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Jung, Myung-ho
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
Egypt, Mansoura
Mansoura University
Abdel-Maksoud, Mohammed S.
South Korea, Seoul
Korea Institute of Science and Technology
South Korea, Daejeon
University of Science and Technology Ust
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: 27
Authors: 6
Affiliations: 3
Identifiers
Doi:
10.1016/j.bmcl.2012.05.004
ISSN:
0960894X
e-ISSN:
14643405