Induction of microtubule stabilization (unknown origin) at 0.2 to 5 uM
- Deposit:2024-05-03
- Modify:2024-05-03
Title: Dual targeted 2-Benzylideneindanone pendant hydroxamic acid group exhibits selective HDAC6 inhibition along with tubulin stabilization effect.
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 (IC50, 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.
Journal: Bioorg Med Chem
Year: 2023
Volume: 86
First Page: 117300
Last Page: 117300
DOI: 10.1016/j.bmc.2023.117300
Target ChEMBL ID: CHEMBL2095182
ChEMBL Target Name: Tubulin
ChEMBL Target Type: PROTEIN COMPLEX GROUP - Target is a poorly defined protein complex, where subunit composition is unclear (e.g., GABA-A receptor)
Relationship Type: D - Direct protein target assigned
Confidence: Multiple direct protein targets may be assigned
- PubChem
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