Synthesis, biological evaluation, and molecular docking studies of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives as anticancer agents

Bioorganic & Medicinal Chemistry Letters
Xi LiHai-Liang Zhu

Abstract

A series of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives have been designed, synthesized and evaluated for their potential antiproliferation activity and Aurora-A kinase inhibitory activity. Among all the compounds, compound 10e possessed the most potent biological activity against HCT116 and MCF-7 cell lines with IC(50) values of 0.39±0.06μM and 0.46±0.04 μM, respectively, which were comparable to the positive control. Compound 10e also exhibited significant Aurora-A kinase inhibitory activity (IC(50)=0.16±0.03 μM). Docking simulation was performed to position compound 10e into the active site of Aurora-A kinase, in order to get the probable binding model for further study. The results of Western-blot assay demonstrated that compound 10e possessed good Aurora-A kinase inhibitory activity against HCT116. Based on the preliminary results, it is deduced that compound 10e with potent Aurora-A kinase inhibitory activity may be a potential anticancer agent.

References

Jan 5, 2005·Nature Reviews. Cancer·Bruce A Chabner, Thomas G Roberts
Feb 3, 2005·Nature Reviews. Molecular Cell Biology·Satyajit K MitraDavid D Schlaepfer
Nov 30, 2005·Cellular and Molecular Life Sciences : CMLS·S HonoreD Braguer
Oct 27, 2007·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Om PrakashAjay Kumar

❮ Previous
Next ❯

Citations

Feb 11, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mostafa M GhorabMohammad K Parvez
Mar 4, 2015·International Journal of Medicinal Chemistry·Prasanna A Datar, Sonali R Jadhav
Oct 29, 2013·European Journal of Medicinal Chemistry·Harish KumarNeelam Jain
May 19, 2016·European Journal of Medicinal Chemistry·Mohemmed Faraz KhanMohammad Shaquiquzzaman
Jan 13, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Khalid KarrouchiM'hammed Ansar
Sep 9, 2015·Organic & Biomolecular Chemistry·T Srinivasa ReddyRavi Shukla
Feb 8, 2019·Anti-cancer Agents in Medicinal Chemistry·Magda M F IsmailMarwa F Harras
Sep 20, 2017·Future Medicinal Chemistry·Mostafa Mm El-MiligyMarwa M Abu-Serie
May 22, 2021·European Journal of Medicinal Chemistry·Tathagata PradhanVikramdeep Monga

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.