A novel series of pyrazole derivatives containing hydroxamic acid group were designed and synthesized as multi-target inhibitors targeting CDK2 (cyclin-dependent kinases 2) and HDAC (histone deacetylase). Compounds 6e and 6f exhibited most potent CDK2 inhibition as well as HDAC inhibition. In vitro antiproliferative assay indicated that several compounds showed better antiproliferative potency compared to olomoucine and SAHA. Docking simulation suggested a common mode of interaction at the active binding sites of CDK2 and HDAC, which demonstrates that compound 6f is a potential agent for cancer therapy deserving further researching.
| Published in | Journal of Drug Design and Medicinal Chemistry (Volume 2, Issue 4) |
| DOI | 10.11648/j.jddmc.20160204.12 |
| Page(s) | 40-46 |
| Creative Commons |
This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited. |
| Copyright |
Copyright © The Author(s), 2016. Published by Science Publishing Group |
Pyrazole, CDK2, HDAC, Inhibior, Anticancer
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APA Style
Xianfeng Huang, Bei Yang, Yuanyuan Liu, Cheng Zhang, Guoqiang Song. (2016). Synthesis and Biological Evaluation of 3-Aryl Pyrazoles as CDK2/HDAC Inhibitor for Anticancer Agents. Journal of Drug Design and Medicinal Chemistry, 2(4), 40-46. https://doi.org/10.11648/j.jddmc.20160204.12
ACS Style
Xianfeng Huang; Bei Yang; Yuanyuan Liu; Cheng Zhang; Guoqiang Song. Synthesis and Biological Evaluation of 3-Aryl Pyrazoles as CDK2/HDAC Inhibitor for Anticancer Agents. J. Drug Des. Med. Chem. 2016, 2(4), 40-46. doi: 10.11648/j.jddmc.20160204.12
AMA Style
Xianfeng Huang, Bei Yang, Yuanyuan Liu, Cheng Zhang, Guoqiang Song. Synthesis and Biological Evaluation of 3-Aryl Pyrazoles as CDK2/HDAC Inhibitor for Anticancer Agents. J Drug Des Med Chem. 2016;2(4):40-46. doi: 10.11648/j.jddmc.20160204.12
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Download@article{10.11648/j.jddmc.20160204.12,
author = {Xianfeng Huang and Bei Yang and Yuanyuan Liu and Cheng Zhang and Guoqiang Song},
title = {Synthesis and Biological Evaluation of 3-Aryl Pyrazoles as CDK2/HDAC Inhibitor for Anticancer Agents},
journal = {Journal of Drug Design and Medicinal Chemistry},
volume = {2},
number = {4},
pages = {40-46},
doi = {10.11648/j.jddmc.20160204.12},
url = {https://doi.org/10.11648/j.jddmc.20160204.12},
eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.jddmc.20160204.12},
abstract = {A novel series of pyrazole derivatives containing hydroxamic acid group were designed and synthesized as multi-target inhibitors targeting CDK2 (cyclin-dependent kinases 2) and HDAC (histone deacetylase). Compounds 6e and 6f exhibited most potent CDK2 inhibition as well as HDAC inhibition. In vitro antiproliferative assay indicated that several compounds showed better antiproliferative potency compared to olomoucine and SAHA. Docking simulation suggested a common mode of interaction at the active binding sites of CDK2 and HDAC, which demonstrates that compound 6f is a potential agent for cancer therapy deserving further researching.},
year = {2016}
}
TY - JOUR T1 - Synthesis and Biological Evaluation of 3-Aryl Pyrazoles as CDK2/HDAC Inhibitor for Anticancer Agents AU - Xianfeng Huang AU - Bei Yang AU - Yuanyuan Liu AU - Cheng Zhang AU - Guoqiang Song Y1 - 2016/08/01 PY - 2016 N1 - https://doi.org/10.11648/j.jddmc.20160204.12 DO - 10.11648/j.jddmc.20160204.12 T2 - Journal of Drug Design and Medicinal Chemistry JF - Journal of Drug Design and Medicinal Chemistry JO - Journal of Drug Design and Medicinal Chemistry SP - 40 EP - 46 PB - Science Publishing Group SN - 2472-3576 UR - https://doi.org/10.11648/j.jddmc.20160204.12 AB - A novel series of pyrazole derivatives containing hydroxamic acid group were designed and synthesized as multi-target inhibitors targeting CDK2 (cyclin-dependent kinases 2) and HDAC (histone deacetylase). Compounds 6e and 6f exhibited most potent CDK2 inhibition as well as HDAC inhibition. In vitro antiproliferative assay indicated that several compounds showed better antiproliferative potency compared to olomoucine and SAHA. Docking simulation suggested a common mode of interaction at the active binding sites of CDK2 and HDAC, which demonstrates that compound 6f is a potential agent for cancer therapy deserving further researching. VL - 2 IS - 4 ER -
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