Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways.

doi:10.1016/j.bmcl.2010.06.030

Paper

Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways.

Published Aug 1, 2010 · Qianbin Li, Jingde Wu, Hui Zheng

Bioorganic & medicinal chemistry letters

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Abstract

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Study Snapshot

The compound 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione shows potential as a dual signaling pathway inhibitor and anticancer agent by inhibiting cell proliferation and inducing early apoptos

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways.

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References

Citations

Structure–Activity Relationship Study and Design Strategies of Hydantoin, Thiazolidinedione, and Rhodanine-Based Kinase Inhibitors: A Two-Decade Review

Hydantoin, thiazolidinedione, and rhodanine-based kinase inhibitors show promise in targeted cancer therapy due to their ability to inhibit kinase activity and their structural insights into their future development.

Design, synthesis, biological evaluations and in silico studies of N-substituted 2,4-thiazolidinedione derivatives as potential a-glucosidase inhibitors.

N-substituted 2,4-thiazolidinedione derivatives show potential as -glucosidase inhibitors, with compounds A-12 and A-14 showing the most potent activity and being non-toxic in cytotoxicity studies.

3-(2-Diisopropylaminoethyl)-5-(4-methoxybenzylidene)thiazolidine-2,4-dione

The novel non-condensed thiazolidine-2,4-dione-bearing derivative was synthesized using a cost-effective two-step approach, providing potential for medicinal chemistry applications.

3-Phenylpropanal and citral in the multicomponent synthesis of novel thiopyrano[2,3-d]thiazoles

3-phenylpropanal selectively forms novel thiopyrano[2,3-d]thiazoles, while citral produces a mixture of two products and Michael adducts, suggesting a one-pot/two-steps protocol for citral transformation.

Research progress of MEK1/2 inhibitors and degraders in the treatment of cancer.

Proteolysis targeting chimera (PROTAC) technology, which induces MEK1/2 degradation, offers a promising cancer therapy strategy, but long-term application is limited due to acquired resistance.

A novel dual MEK/PDK1 inhibitor 9za retards the cell cycle at G0/G1 phase and induces mitochondrial apoptosis in non-small cell lung cancer cells

The novel dual MEK/PDK1 inhibitor 9za effectively inhibits cell growth and induces apoptosis in non-small cell lung cancer cells, offering a potential treatment option for this cancer.

Dual inhibitors of RAF-MEK-ERK and PI3K-PDK1-AKT pathways: Design, synthesis and preliminary anticancer activity studies of 3-substituted-5-(phenylamino) indolone derivatives.

Dual-pathway inhibitors, such as 9za, show potential for effective lung cancer therapy by blocking RAF-MEK-ERK and PI3K-PDK1-AKT pathways.

Ocular Toxicity Profile of ST-162 and ST-168 as Novel Bifunctional MEK/PI3K Inhibitors.

ST-162 and ST-168 show favorable in vitro and in vivo ocular toxicity profiles, supporting their further development as potential therapeutic agents targeting multiple aggressive tumors.

5-Ene-4-thiazolidinones – An efficient tool in medicinal chemistry

5-ene-4-thiazolidinones are a widely studied class in medicinal chemistry, with their pharmacological effects influenced by the presence/nature of C5 substituents.