Design, synthesis and biological evaluation of novel 2,3-indolinedione derivatives against mantle cell lymphoma

Bioorg Med Chem. 2019 Aug 1;27(15):3319-3327. doi: 10.1016/j.bmc.2019.06.009.

Shengping Yu ¹, Yang Liu ², Zhen Zhang ¹, Jingya Zhang ¹, Guisen Zhao ³

Affiliations

1 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, PR China.
2 Department of Lymphoma and Myeloma, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.
3 Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, PR China. Electronic address: guisenzhao@sdu.edu.cn.

PMID: 31229421 DOI: 10.1016/j.bmc.2019.06.009

Abstract

2,3-Indolinedione derivatives have been identified as a novel class of promising agents for Cancer treatment. In this study, eighteen 2,3-indolinedione derivatives were designed and synthesized, and their Anticancer activities against mantle cell lymphoma (MCL) cells were evaluated. Most of them exhibited significant antiproliferative activity against the tested cell lines, and compound K5 was the most potent (MCL cellular IC₅₀ = 0.4-0.7 μM). Further, compound K5 could induce cell Apoptosis and cell cycle arrest in G2/M phase. Additionally, the results of drug-likeness analysis demonstrated that these novel 2,3-indolinedione derivatives could have potential as novel treatment strategies for MCL.

Keywords

2,3-Indolinedione; Biological activities; Derivatives; Mantle cell lymphoma.

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