Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity |
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| Authors: | Shravankumar Kankala Koteshwar Rao Rama Chekrapani Kesari Fredrik Björkling Srinivas Nerella Prasad Gundepaka |
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| Affiliation: | 1. Department of Chemistry, Kakatiya University, Warangal, Telangana, India shravankankala@yahoo.com!["ORCID]("//:0" "\"ORCID") https://orcid.org/0000-0002-1398-7620;3. Department of Chemistry, Mewar University, Chittorgarh, Rajasthan, India;4. Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark;5. Department of Chemistry, Kakatiya University, Warangal, Telangana, India https://orcid.org/0000-0003-3750-8206;6. Centre for Pharmaceutical Science, Institute of Science and Technology, JNTU, Hyderabad, India |
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| Abstract: | 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. |
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| Keywords: | Fluorophenylpyrazole-picolinamide cross-coupling palladium-N-heterocyclic carbenes anticancer activity |
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!["ORCID]({"type":"image","src":"/templates/jsp/images/orcid.png"} "\"ORCID")
https://orcid.org/0000-0002-1398-7620;3. Department of Chemistry, Mewar University, Chittorgarh, Rajasthan, India;4. Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark;5. Department of Chemistry, Kakatiya University, Warangal, Telangana, India