Synthesis and antiproliferative activity of thiazolidine analogs for melanoma

doi:10.1016/j.bmcl.2007.05.059

Bioorganic & Medicinal Chemistry Letters

Volume 17, Issue 15, 1 August 2007, Pages 4113-4117

https://doi.org/10.1016/j.bmcl.2007.05.059 Get rights and content

Abstract

We have previously described 2-aryl-thiazolidine-4-carboxylic acid amides as a novel class of antiproliferative agents for prostate cancer. Screening these compounds with melanoma cell lines revealed that several of them have potent antiproliferative activity and selectivity against melanoma. To further improve the potency and selectivity, we synthesized a new series of analogs and tested them in two melanoma cell lines and fibroblast cells (negative controls). Comparison of anticancer effects of these compounds with a standard chemotherapeutic agent, sorafenib, showed that they are very effective in killing melanoma cells with low micromolar to nanomolar antiproliferative activity and provide us a new lead for developing potential drugs for melanoma.

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Acknowledgments

This research is supported by funds from Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center (W.L.), and the Van Vleet Endowed Professorship (D.D.M.). We thank Dr. David L. Armbruster for editorial assistance.

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Synthesis and antiproliferative activity of thiazolidine analogs for melanoma

Abstract

Graphical abstract

Section snippets

Acknowledgments

J. Am. Acad. Dermatol.

Clin. Oncol. (R. Coll. Radiol.)

Eur. J. Cancer

Eur. J. Cancer

Bioorg. Med. Chem. Lett.

Tetrahedron

Farmaco

CA Cancer J. Clin.

Curr. Oncol. Rep.

Oncology (Williston Park)

J. Exp. Clin. Cancer Res.

Cancer Control

J. Clin. Oncol.

Melanoma Res.