Design, synthesis and anti-cancer evaluation of a novel series of pyrazolo [1, 5-a] pyrimidine substituted diamide derivatives

A novel series of pyrazolo [1, 5-a] pyrimidine substituted diamides has been designed and synthesized using a linear mode multistep synthesis. The synthesized compounds were characterized by 1 H NMR, 13 C NMR, ESI-MS and IR analyses. These new compounds were screened for their in vitro antiprolifera...

Full description

Saved in:
Bibliographic Details
Published in:Medicinal chemistry research 2017-04, Vol.26 (4), p.714-744
Main Authors: Ajeesh Kumar, A.K., Bodke, Yadav D., Lakra, Peter Serjious, Sambasivam, Ganesh, Bhat, Kishore G.
Format: Article
Language:English
Subjects:
Anticancer properties
Antitumor activity
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
NMR
Nuclear magnetic resonance
Original Research
Pharmacology/Toxicology
Pyrimidines
Substitutes
Synthesis
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A novel series of pyrazolo [1, 5-a] pyrimidine substituted diamides has been designed and synthesized using a linear mode multistep synthesis. The synthesized compounds were characterized by 1 H NMR, 13 C NMR, ESI-MS and IR analyses. These new compounds were screened for their in vitro antiproliferative activity using an MTT assay. Out of 23 derivatives synthesized in the current study, compounds 10q , 10u and 10w showed good anticancer activity against HeLa cell line. Furthermore, these derivatives gave IC 50 values of less than 10 µM against HeLa cell and were therefore more potent than the marketed anticancer drug cis-platin (17.83 µM).
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-016-1770-0