AI Article Synopsis
- Abnormal epigenetics, particularly the acetylation of lysine, plays a significant role in tumor progression, making it a target for anticancer drug development.
- Current HDAC inhibitors face challenges like toxicity and drug resistance, prompting research into new compounds.
- The study focused on bivalent indanone-based ligands, finding that analogues 9 and 21 have strong antiproliferative properties and high potency against the HDAC 6 enzyme, with potential dual benefits of microtubule stabilization and anti-inflammatory effects.
Article Abstract
Abnormal epigenetics has been recognised as an early event in tumour progression and aberrant acetylation of lysine in particular has been understood in tumorigenesis. Therefore, it has become an attractive target for anticancer drug development. However, HDAC inhibitors have limited success due to toxicity and drug resistance concerns. Present study deals with design and synthesis of bivalent indanone based HDAC6 and antitubulin ligands as anticancer agents. Two of the analogues 9 and 21 exhibited potent antiproliferative activities (IC, 0.36-3.27 µM) and high potency against HDAC 6 enzyme. Compound 21 showed high selectivity against HDAC 6 while 9 exhibited low selectivity. Both the compounds also showed microtubule stabilization effects and moderate anti-inflammatory effect. Dual targeted anticancer agents with concomitant anti-inflammatory effects will be more attractive clinical candidates in future.
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| http://dx.doi.org/10.1016/j.bmc.2023.117300 | DOI Listing |
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