Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents

Saravanan, K. and Elancheran, R. and Divakar, S. and Anand, S. Athavan Alias and Ramanathan, M. and Kotoky, Jibon and Lokanath, N. K. and Kabilan, S. (2017) Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents. Bioorganic & Medicinal Chemistry Letters, 27 (5). 1199 - 1204. ISSN 0960-894X

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Official URL: https://doi.org/10.1016/j.bmcl.2017.01.065

Abstract

The structural modification and molecular docking-based screening approaches on thiazole-based isoindolinediones were imposed to find the novel 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives. The best fit compounds (6a-n) were synthesized and evaluated their antiproliferative activities on the prostate cancer cell lines (PC-3 & LNCaP). Among them, the compound, 6m exhibited good activity, particularly on LNCaP (IC50=5.96±1.6μM), moderately active against PC-3 cell lines as compared to bicalutamide. The compound, 6m decreased the androgen-mediated transcription of ARE-mRNA in PSA, TMPRSS2, c-myc and cyclin D1 than R-bicalutamide. The compounds, 6e and 6f were reconfirmed through single crystal XRD analysis. The ADME profiling of the test compounds was evaluated to find the drug-likeness and pharmacokinetic parameters. These findings may provide vital information for the development of anti-prostate cancer agents.

Item Type: Article
Uncontrolled Keywords: Androgen receptor, Prostate cancer, AR antagonist, Isoindolinediones, Molecular docking
Subjects: D Physical Science > Physics
Divisions: Department of > Physics
Depositing User: MUL SWAPNA user
Date Deposited: 25 Jun 2019 06:01
Last Modified: 28 Jun 2019 09:19
URI: http://eprints.uni-mysore.ac.in/id/eprint/3799

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