Design and synthesis of new [1,2,3]Triazolo[4,5-d]pyrimidine derivatives as potential antiproliferative agents

Title
Design and synthesis of new [1,2,3]Triazolo[4,5-d]pyrimidine derivatives as potential antiproliferative agents
Authors
Ahmed Mahammed ElkamhawyAl-Sanea, Mohammad M송치만심태보노은주
Keywords
pyrimide골격포함; 세포주기반 항암활성; NCI 항암세포활성검색; FGFR효소활성; Antiproliferative activity; [1,2,3]Triazolo[4,5-d]pyrimidine; NCI 60 cell lines panel; FGFR3 kinase
Issue Date
2015-07
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 36, NO 7, 1863-1873
Abstract
A new series possessing [1,2,3]triazolo[4,5-d]pyrimidine scaffold was synthesized and biologically evaluated for potential antiproliferative activity. Fourteen compounds were selected for in vitro anticancer assay over a panel of 60 cell lines at National Cancer Institute (NCI), USA. The most sensitive cell lines to the synthesized compounds were leukemia (K-562 and SR), nonsmall cell lung cancer HOP-92, and melanoma MDA-MB-435. Compounds 12 and 24 exerted broad spectrum activity against most cell panel, while compounds 14, 21, and 23 exhibited effectiveness toward specific cell lines belong to different tumor subpanels. Accordingly, SAR, COMPARE analyses, and in silicoADME profiling were discussed for the target compounds. In addition, compounds 11 and 22 exerted good FGFR3 inhibitory activity with 58.8 and 46.7% at 100 M, respectively. Taken as a whole, the present study revealed that the new series can be considered as promising lead for further development of more potent anticancer agents as well as FGFR3 kinase potential inhibitors.
URI
http://pubs.kist.re.kr/handle/201004/50793
ISSN
02532964
Appears in Collections:
KIST Publication > Article
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