title: Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
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.
authors: Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo, Spain.
authors: Patricia
authors: P
authors: García-Domínguez
authors: Carmela
authors: C
authors: Dell'aversana
authors: Rosana
authors: R
authors: Alvarez
authors: Lucia
authors: L
authors: Altucci
authors: Angel R
authors: AR
authors: de Lera
mesh_terms: D000634:Aminoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002384:Catalysis; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D004248:DNA (Cytosine-5-)-Methyltransferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007938:Leukemia / Q000201:enzymology / Q000473:pathology; D010165:Palladium / Q000737:chemistry; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020298:U937 Cells
chemical_list: D000634:Aminoquinolines; D004791:Enzyme Inhibitors; D011743:Pyrimidines; C581203:SGI-1027; D010165:Palladium; D004248:DNA (Cytosine-5-)-Methyltransferases