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Induction of microtubule stabilization (unknown origin) at 0.2 to 5 uM

PubChem AID
1956035
Primary Citation
Dual targeted 2-Benzylideneindanone pendant hydroxamic acid group exhibits selective HDAC6 inhibition along with tubulin stabilization effect [PMID: 37146520]
Source
External ID
Tested Substances
Tested Compounds
Version
1.1
Status
Live
Dates
  • Deposit:
    2024-05-03
  • Modify:
    2024-05-03
Description
This bioassay record (AID 1956035) reports results from the above primary citation. Additional data from the same publication are reported in a total of 87 BioAssay records in PubChem.

1 Description

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.

2 Comment

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

3 Result Definitions

4 Data Table

5 Target

3 of 15
4 of 15
5 of 15
6 of 15
7 of 15
8 of 15
9 of 15
10 of 15
11 of 15
12 of 15
13 of 15
14 of 15
15 of 15

8 Identity

8.1 BioAssay Name

Induction of microtubule stabilization (unknown origin) at 0.2 to 5 uM

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 Deposit Date

2024-05-03

8.6 Modify Date

Version 1.1
2024-05-03 (currently shown)

8.7 Status

Live

9 Same-Publication BioAssays

10 BioAssay Annotations

Assay Type
Binding
Assay Organism

11 Information Sources

  1. PubChem
  2. ChEMBL
    LICENSE
    Access to the web interface of ChEMBL is made under the EBI's Terms of Use (http://www.ebi.ac.uk/Information/termsofuse.html). The ChEMBL data is made available on a Creative Commons Attribution-Share Alike 3.0 Unported License (http://creativecommons.org/licenses/by-sa/3.0/).
    http://www.ebi.ac.uk/Information/termsofuse.html
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