Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities

Authors

Anil Kumar, University of Rhode Island
Israr Ahmad
Bhupender S. Chhikara, University of Rhode Island
Rakesh Tiwari, University of Rhode Island
Deendayal Mandal, University of Rhode Island
Keykavous Parang, University of Rhode IslandFollow

Document Type

Article

Date of Original Version

2011

Department

Biomedical and Pharmaceutical Sciences

Abstract

A series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC₅₀ value of 5.6 μM. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 μM.

[Refer to PDF for graphical abstract portion]

Citation/Publisher Attribution

Kumar, A., Ahmad, I., Chhikara, B. S., Tiwari, R., Mandal, D., & Parang, K. (2011). Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities. Bioorganic & Medicinal Chemistry Letters, 21(5), 1342-1346. doi: 10.1016/j.bmcl.2011.01.047

Available at: https://doi.org/10.1016/j.bmcl.2011.01.047

Creative Commons License

This work is licensed under a Creative Commons Attribution-Noncommercial-No Derivative Works 4.0 License.