AI Article Synopsis
- Histone deacetylases (HDACs) are key targets for cancer therapy, prompting the urgent need for new HDAC inhibitors (HDACis).
- Researchers designed and synthesized new compounds called aroylpiperazine hybrid derivatives, specifically focusing on indole-piperazine hybrids 6a and 6b.
- The compound 6a demonstrated strong activity against HDAC1 with an IC value of 205 nM and showed better cancer cell growth inhibition compared to the existing drug chidamide.
Article Abstract
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 (IC = 205 nM) and 6b (IC = 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.
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| http://dx.doi.org/10.1248/cpb.c22-00635 | DOI Listing |
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