Discovery of Indole-Piperazine Hybrid Structures as Potent Selective Class I Histone Deacetylases Inhibitors
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- Xing Liang
- Guangxi Key Laboratory of Urban Water Environment, College of Chemistry and Environmental Engineering, Baise University
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- Gong Guoliang
- Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University
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- Chen Xinyang
- Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University
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- Chen Xin
- Shaanxi Key Labotory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University
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Abstract
<p>Histone deacetylases (HDACs) are important targets in cancer treatment, and the development of selective and broad-spectrum HDACs inhibitors (HDACis) is urgent. In this research, a series of aroylpiperazine hybrid derivatives were designed and synthesized. Among these, indole-piperazine hybrids 6a (IC50 = 205 nM) and 6b (IC50 = 280 nM) showed submicromolar activity against HDAC1. Moreover, 6a showed a preferable affinity toward class I HDACs, especially for HDAC1–3. In vitro, 6a exhibited better antiproliferative activities against K562 and HCT116 cell lines than chidamide.</p>
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 71 (3), 206-212, 2023-03-01
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390295270227997824
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- ISSN
- 13475223
- 00092363
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- Text Lang
- en
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- Data Source
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- JaLC
- Crossref
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- Abstract License Flag
- Disallowed