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

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

Year of Publication: 2019
Contained in: Future medicinal chemistry Vol. 11, No. 14 (2019), p. 1679-1702
All journal articles: Search for all articles in this journal
Language: English
Contributors: Dutta, Sanchita | Author
Halder, Amit Kumar
Adhikari, Nilanjan
Amin, Sk Abdul
Das, Sanjib
Saha, Achintya
Jha, Tarun
Full text access:
Electronic availability is being checked...
Links: Full Text (dx.doi.org)
Keywords: Journal Article
SAR
apoptosis
cell cycle
cytotoxicity
flow cytometry
leukemia
metalloenzyme
mitochondrial membrane potential
molecular docking
pentanoic acid
ISSN: 1756-8927
Note: Copyright: From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Notes: Date Revised 10.09.2019
published: Print-Electronic
Citation Status In-Data-Review
Copyright: From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Physical Description: Online-Ressource
ID (e.g. DOI, URN): 10.4155/fmc-2018-0361
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