Substituted 6-amino-4H-[1,2]dithiolo[4,3-b]pyrrol-5-ones: Synthesis, structure-activity relationships, and cytotoxic activity on selected human cancer cell lines
Document Type
Article
Publication Date
7-1-2007
Abstract
An efficient synthesis and the cytotoxic activity of a series of substituted 6-amino-4H-[1,2]dithiolo[4,3-b]pyrrol-5-ones 1a-q is described. The synthesis was accomplished in an expedient manner (seven-steps) from commercially available starting materials. Several of the derivatives tested demonstrated significant in vitro cytotoxic activity against the human cancer cell lines H460 (≥7 nM) and LCC6 (≥28 nM). Following SAR and pharmacokinetic studies a derivative was further evaluated for its in vivo anti-tumor activity against a highly angiogenic human melanoma xenograft where it demonstrated significant efficacy as a mono-therapy and in combination with Taxol and Cisplatin. © 2007 Elsevier Ltd. All rights reserved.
Publication Source (Journal or Book title)
Bioorganic and Medicinal Chemistry
First Page
4601
Last Page
4608
Recommended Citation
Li, B., Lyle, M., Chen, G., Li, J., Hu, K., Tang, L., Alaoui-Jamali, M., & Webster, J. (2007). Substituted 6-amino-4H-[1,2]dithiolo[4,3-b]pyrrol-5-ones: Synthesis, structure-activity relationships, and cytotoxic activity on selected human cancer cell lines. Bioorganic and Medicinal Chemistry, 15 (13), 4601-4608. https://doi.org/10.1016/j.bmc.2007.04.017