Diarylureas and Diarylamides with Pyrrolo[2,3-d]pyrimidine Scaffold as Broad-Spectrum Anticancer Agents

Title
Diarylureas and Diarylamides with Pyrrolo[2,3-d]pyrimidine Scaffold as Broad-Spectrum Anticancer Agents
Authors
모하메드엘가말오창현
Keywords
pyrrolo[2,3-d]pyrimidine; anticancer; cytotoxicity; diarylurea; diarylamide
Issue Date
2014-01
Publisher
Chemical & pharmaceutical bulletin
Citation
VOL 62, NO 1, 25-34
Abstract
A series of diarylureas and diarylamides possessing pyrrolo[2,3-d]pyrimidine scaffold was designed and synthesized. The in vitro antiproliferative activities of a selected group of the target compounds against NCI-60 cell line panel were tested and compared with Sorafenib and Imatinib as reference compounds. Most of the compounds showed strong and broad-spectrum antiproliferative activities. Compounds IVa, IVb, and IVd with benzamido moiety at position 4 of the pyrrolo[2,3-d]pyrimidine nucleus, para-disubstituted phenyl ring at N1-position of pyrrolo[2,3-d]pyrimidine scaffold, and urea linker showed strong and broad-spectrum anticancer results with high potencies and efficacies. In addition, the amide derivatives Vb and Vc demonstrated one-digit nanomolar IC50 values over two and one cell line(s), respectively. Amid all the target compounds, compound IVa demonstrated the best results in both one-dose and five-dose testing modes. It showed 109.18% mean % inhibition over the NCI-60 cancer cell line panel at 10 μM concentration, submicromolar 50% inhibitory concentration (IC50) values over eight cell lines of eight different cancer types, and high efficacy with total growth inhibition (TGI) and 50% lethal concentration (LC50) values less than 4.22 μM over three colon, ovarian, and prostate cancer cell lines. It showed superior potency and efficacy to Sorafenib and Imatinib over most of the tested cell lines.
URI
http://pubs.kist.re.kr/handle/201004/48179
ISSN
00092363
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