Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents

Bioorganic & Medicinal Chemistry
Peng-Cheng LvHai-Liang Zhu

Abstract

Two series of pyrazole derivatives designing for potential EGFR kinase inhibitors have been discovered. Some of them exhibited significant EGFR inhibitory activity. Compound 3-(3,4-dimethylphenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (C5) displayed the most potent EGFR inhibitory activity with IC₅₀ of 0.07 μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the pyrazole derivatives own high antiproliferative activity against MCF-7. Compound C5 showed significant antiproliferative activity against MCF-7 with IC₅₀ of 0.08 μM. Therefore, compound C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.

References

Apr 20, 1990·Cell·A Ullrich, J Schlessinger

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Citations

Aug 29, 2013·Organic and Medicinal Chemistry Letters·Poonam KhloyaPawan K Sharma
Oct 25, 2011·PLoS Computational Biology·Shun-Chieh YangCalvin Yu-Chian Chen
Mar 10, 2016·Journal of Pharmacy & Bioallied Sciences·Mohd Javed NaimPerwaiz Alam
Jan 7, 2014·Expert Opinion on Therapeutic Patents·Si-Ning Li, Huan-Qiu Li
Aug 17, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Hai-Chao WangHai-Liang Zhu
Oct 21, 2016·Pharmacognosy Magazine·Preeti RawatMahesh Pal
Feb 18, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jingzi LiuBin He
Feb 8, 2019·Journal of Enzyme Inhibition and Medicinal Chemistry·Raja Solomon ViswasHoyun Lee
Jun 13, 2012·Chemical & Pharmaceutical Bulletin·Azza Taher TaherYasser Mohamed Ragab
Oct 12, 2012·Dalton Transactions : an International Journal of Inorganic Chemistry·Bhajan LalFazlul Huq
Feb 19, 2016·Magnetic Resonance in Chemistry : MRC·Yearam JungYoongho Lim
Mar 23, 2017·Nucleosides, Nucleotides & Nucleic Acids·Ibrahim F NassarNasser S M Ismail
Sep 12, 2020·Bioscience Reports·Rawan Al-SahebOmar S Abu Abed
Nov 12, 2013·Archiv der Pharmazie·Nabhubygari Mahaboob BashaTartte Vijaya
Aug 24, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ibrahim Ali M Radini
Dec 21, 2013·ChemSusChem·Manoj B GawandeRajender S Varma
May 31, 2019·Chemical Biology & Drug Design·Serpil DemirciAyşegül Doğan
Feb 19, 2019·Steroids·Nanuli Sh NadaraiaMarina Sokovic
Dec 31, 2016·ACS Omega·Anusha SebastianKanchugarakoppal S Rangappa
Aug 28, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mohamed RamadanStefan Bräse

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