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

Future Medicinal Chemistry
Sanchita DuttaTarun Jha

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.

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Citations

Jun 22, 2020·European Journal of Medicinal Chemistry·Sk Abdul Amin, Tarun Jha
Dec 7, 2020·European Journal of Medicinal Chemistry·Sandip Kumar BaidyaTarun Jha
Jun 23, 2021·European Journal of Medicinal Chemistry·Sanjib DasTarun Jha

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Methods Mentioned

BETA
NMR
flow cytometry
flow
Fluorescence imaging

Software Mentioned

Maestro
SPSS
FACSDIVA
Mass Hunter Quantitative Analysis

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