Discovery of novel 2,4-diarylaminopyrimidine hydrazone derivatives as potent anti-thyroid cancer agents capable of inhibiting FAK
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| Publicado en: | Journal of Enzyme Inhibition and Medicinal Chemistry vol. 39, no. 1 (Dec 2024) |
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| Autor principal: | |
| Otros Autores: | , , , , , , , , |
| Publicado: |
Taylor & Francis Ltd.
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| Acceso en línea: | Citation/Abstract Full Text - PDF |
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| 001 | 3149476916 | ||
| 003 | UK-CbPIL | ||
| 022 | |a 1475-6366 | ||
| 022 | |a 1475-6374 | ||
| 022 | |a 8755-5093 | ||
| 024 | 7 | |a 10.1080/14756366.2024.2423875 |2 doi | |
| 035 | |a 3149476916 | ||
| 045 | 2 | |b d20241201 |b d20241231 | |
| 100 | 1 | |a Li, Hongting |u Department of Thyroid Surgery, the First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan Province, China | |
| 245 | 1 | |a Discovery of novel 2,4-diarylaminopyrimidine hydrazone derivatives as potent anti-thyroid cancer agents capable of inhibiting FAK | |
| 260 | |b Taylor & Francis Ltd. |c Dec 2024 | ||
| 513 | |a Journal Article | ||
| 520 | 3 | |a In this work, thirty 2,4-diarylaminopyrimidine-based hydrazones were designed, synthesised, and their anti-thyroid cancer activity were explored. The majority of compounds exhibit moderate to excellent cytotoxic activity against FAK overexpressing TPC-1 cells, with IC50 values ranging from 0.113 to 1.460 μM. Among them, compound 14f displayed exceptional anti-proliferative effect against TPC-1 cells (IC50 = 0.113 μM) and potent FAK inhibitory potency (IC50 = 35 nM). In silico studies indicated that compound 14f could well bind to FAK (Focal Adhesion Kinase) and have favourable pharmacokinetic profiles. In addition, compound 14f could inhibit the phosphorylation of FAK at Tyr397, Tyr576/577 and Tyr925, and did not affect the expression level of FAK in TPC-1 cells. Compound 14f was also effective in inhibiting the proliferation and migration of thyroid cancer cells TPC-1. Thus, these novel 4-arylaminopyrimidine hydrazone derivatives exhibited potent anti-thyroid cancer activities through the inhibition of FAK. | |
| 653 | |a Cytotoxicity | ||
| 653 | |a Cell migration | ||
| 653 | |a Thyroid cancer | ||
| 653 | |a Phosphorylation | ||
| 653 | |a Pharmacokinetics | ||
| 653 | |a Focal adhesion kinase | ||
| 653 | |a Cell proliferation | ||
| 653 | |a Thyroidectomy | ||
| 653 | |a Hydrogen bonds | ||
| 653 | |a Pharmaceutical sciences | ||
| 653 | |a Cancer therapies | ||
| 653 | |a Clinical trials | ||
| 653 | |a Chemistry | ||
| 653 | |a Design | ||
| 653 | |a Enzymes | ||
| 653 | |a Kinases | ||
| 700 | 1 | |a Mei-Qi Jia |u School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, Henan Province, China | |
| 700 | 1 | |a Zhao-Long, Qin |u School of Pharmaceutical Sciences, Institute of Drug Discovery & Development Key, Laboratory of Advanced Drug Preparation Technologies (Ministry of Education), Zhengzhou University, Zhengzhou, Henan Province, China | |
| 700 | 1 | |a Lu, Changliang |u Zhengzhou Xingyuan Foreign Language High School, Zhengzhou, Henan Province, China | |
| 700 | 1 | |a Chu, Weili |u Department of Respiratory and Critical Care Medicine, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan Province, China | |
| 700 | 1 | |a Zhang, Ze |u Department of Respiratory and Critical Care Medicine, The First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan Province, China | |
| 700 | 1 | |a Niu, Jinbo |u The Third Affiliated Hospital of Zhengzhou University, Zhengzhou, China | |
| 700 | 1 | |a Song, Jian |u School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, Henan Province, China | |
| 700 | 1 | |a Sai-Yang, Zhang |u School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, Henan Province, China | |
| 700 | 1 | |a Fu, Lijun |u Department of Thyroid Surgery, the First Affiliated Hospital of Zhengzhou University, Zhengzhou, Henan Province, China | |
| 773 | 0 | |t Journal of Enzyme Inhibition and Medicinal Chemistry |g vol. 39, no. 1 (Dec 2024) | |
| 786 | 0 | |d ProQuest |t Health & Medical Collection | |
| 856 | 4 | 1 | |3 Citation/Abstract |u https://www.proquest.com/docview/3149476916/abstract/embedded/7BTGNMKEMPT1V9Z2?source=fedsrch |
| 856 | 4 | 0 | |3 Full Text - PDF |u https://www.proquest.com/docview/3149476916/fulltextPDF/embedded/7BTGNMKEMPT1V9Z2?source=fedsrch |