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Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line
Patricia García-Domínguez1, Carmela Dell'aversana, Rosana Alvarez
1Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo, Spain.
Bioorganic & Medicinal Chemistry Letters
|February 14, 2013
Abstract:
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.
