Publication Cover
Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 50, 2020 - Issue 19
297
Views
2
CrossRef citations to date
0
Altmetric
Articles

Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity

ORCID Icon, , , , ORCID Icon, , & show all
Pages 2997-3006 | Received 19 Jan 2020, Published online: 15 Jul 2020
 

Abstract

A series of fluorophenylpyrazole-picolinamide derivatives were synthesized in high yields using a cross-coupling reaction catalyzed by in situ formed palladium-N-heterocyclic carbenes (Pd-NHCs). The synthesized novel derivatives were evaluated for in vitro anticancer activity against a panel of four human tumor cell lines, HeLa (cervical), A-549 (lung), MCF-7 (breast), and IMR-32 (neuroblastoma). Four compounds, 11c, 11e, 11j, and 11k, showed growth inhibition (low µM) comparable with the standard drug cisplatin, providing a preliminary structure–activity relationship for the series. The present procedure is operationally simple and works with a wide range of substrates and may thus be useful in further compound optimization.

Graphical Abstract

Acknowledgments

Dr. S. Kankala is thankful to CSIR, New Delhi for the award of Research Associate.

Disclosure statement

No potential conflict of interest was reported by the author(s).

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.