Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line

The known DNMT inhibitor SGI-1027 4 has been synthesized using as key steps Pd-catalyzed Ar–N bond formation reactions performed in a sequential or convergent manner. In the former approach, a by-product, which corresponds to the incorporation of two units of 4-chloroquinoline, was also isolated. The biological effects of compound 4 in the U937 human leukemia cell line are also described.

The quinoline-based compound SGI-1027 has been synthesized using Pd-catalyzed Ar–N bond construction on a sequential or a convergent manner. Its activity as DNMT1 inhibitor and the biological effects in the U937 human leukemia are described.Figure optionsDownload as PowerPoint slide