The synthesis of new planar derivatives characterized by the presence of a pyridothiopyranopyrazole or pyridothiopyranopyrimidine nucleus, carrying a substituted aryl group, is reported. The novel 1,4-dihydropyrido[3′,2′:5,6]thiopyrano[4,3-c]pyrazole derivatives were obtained by condensation of 2,3-dihydro-3-hydroxymethylenethiopyrano[2,3-b]pyridin-4(4H)-ones with appropriate hydrazines. The preparation of 2-substituted pyrido[3′,2′:5,6]thiopyrano[4,3-d]pyrimidines was accomplished from the intermediate 2,3-dihy-dro-3-dimethylaminomethylenethiopyrano[2,3-b]pyridin-4(4H)-ones by reaction with the appropriate binucleophile amidines. The antiproliferative activity of some new products was tested by an in vitro assay on human tumour cell lines (HL-60 and HeLa), but none of them showed any significant effects in the tests performed. Accordingly, linear flow dichroism measurements indicated their inability to form a molecular complex with DNA.
|Autori:||PRIMOFIORE G; MARINI A; DA SETTIMO PASSETTI F; S. SALERNO; D. BERTINI; L. DALLA VIA; S. MARCIANI MAGNO|
|Titolo:||Synthesis of novel 1,4-dihydropyrido[3’,2’:5,6]thiopyrano[4,3-c]-pyrazoles and 5H-pyrido[3’,2’:5,6]thiopyrano[4,3-d]pyrimidines as potential antiproliferative agents|
|Anno del prodotto:||2003|
|Digital Object Identifier (DOI):||10.1002/jhet.5570400506|
|Appare nelle tipologie:||1.1 Articolo in rivista|