Design, synthesis and biological evaluation of novel 1,3-diarylpyrazoles as cyclooxygenase inhibitors, antiplatelet and anticancer agents.

Date

2018-04-06

Author

Inceler, Nazan
ÖZKAN, YEŞİM
Turan, Nilufer Nermin
Kahraman, Deniz Cansen
Atalay, Rengül
BAYTAŞ, Sultan

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With the aim of achieving new compounds possessing both anti-inflammatory and antiplatelet activities, we synthesized (E)-3-[3-(pyridin-3/4-yl)-1-(phenyl/sulfonylmethylphenyl)-1H-pyrazol-4-yl]acrylamides, and evaluated their COX-1 and COX-2 inhibitory and antiplatelet activities. Since COX-2 inhibitory and antiplatelet compounds have anticancer potential, we also screened their antiproliferative effects against three human cancer cell lines. Compounds 5n, 5p, 5s, 10d, 10g and 10i were determined as dual COX-2 inhibitor/antiplatelet compounds. Compound 10h appeared to be a compound that exhibited antiplatelet activity without inhibiting the COX enzyme. Compounds 5h, 10a and 10i were the most effective derivatives which displayed antiproliferative activity against Huh7, MCF7 and HCT116 cells. Particularly, compound 10i, as the compound exhibiting the highest cytotoxic, antiplatelet and COX-2 inhibitory activity, was remarkable.

Subject Keywords

Selective cox-2 inhibitors, Cardiovascular risk, Prostaglandin endoperoxides, Antiinflammatory activities, Breast-cancer, Derivatives, Thromboxane, Expression, Carcinoma, Prostacyclin

URI

https://hdl.handle.net/11511/32359

Journal

MedChemComm

DOI

https://doi.org/10.1039/c8md00022k

Collections

Graduate School of Informatics, Article

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Citation Formats

N. Inceler, Y. ÖZKAN, N. N. Turan, D. C. Kahraman, R. Atalay, and S. BAYTAŞ, “Design, synthesis and biological evaluation of novel 1,3-diarylpyrazoles as cyclooxygenase inhibitors, antiplatelet and anticancer agents.,” MedChemComm, pp. 795–811, 2018, Accessed: 00, 2020. [Online]. Available: https://hdl.handle.net/11511/32359.