Literature DB >> 31370697

Synthesis, anticancer activity, structure-activity relationship and binding mode of interaction studies of substituted pentanoic acids.

Sanchita Dutta1,2, Amit Kumar Halder1, Nilanjan Adhikari1, Sk Abdul Amin1, Sanjib Das1, Achintya Saha2, Tarun Jha1.   

Abstract

Aim: Simultaneous inhibition of MMP-2 and HDAC8 may be an effective strategy to target cancer. Methodology: In continuation of our earlier efforts, a series of substituted pentanoic acids (1-18) were synthesized and checked for their biological activity along with some earlier reported compounds (19 -35).
Results: Compounds 18 and 31 were found to induce apoptosis effectively in a dose-dependent fashion in Jurkat-E6.1 cell line. They reduced the expression of both MMP-2 and HDAC8 effectively. 31 also produced prominent intensity of fluorescence to bring nick in Jurkat-E6.1 cells. 31 also showed cellular arrest in sub-G0 phase.
Conclusion: Such compounds may be useful to battle against cancer.

Entities:  

Keywords:  SAR; apoptosis; cell cycle; cytotoxicity; flow cytometry; leukemia; metalloenzyme; mitochondrial membrane potential; molecular docking; pentanoic acid

Mesh:

Substances:

Year:  2019        PMID: 31370697     DOI: 10.4155/fmc-2018-0361

Source DB:  PubMed          Journal:  Future Med Chem        ISSN: 1756-8919            Impact factor:   3.808


  1 in total

Review 1.  Fight against novel coronavirus: A perspective of medicinal chemists.

Authors:  Sk Abdul Amin; Tarun Jha
Journal:  Eur J Med Chem       Date:  2020-06-12       Impact factor: 6.514

  1 in total

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