Lacova, Margita published the artcileA novel and efficient synthesis of 3-aryl-5-(2-hydroxybenzoyl)pyridin-2(1H)-ones by re-cyclization of N-(oxopyranochromenyl)acetamides and their antineoplastic screening, Category: isoquinoline, the main research area is pyridinone preparation oxopyranochromenyl acetamide recyclization antitumor human.
A novel, simple and efficient methodol. for preparation of yet unknown 3-aryl-5-(2-hydroxybenzoyl)pyridin-2(1H)-ones I (R = H, 9-Me, 9-NO2, 8,9-(Me)2; Ar = Ph, 4-MeO, 4-NO2, 1H-tetrazole) by EtONa driven re-cyclization of N-(3-aryl-2-oxo-2,5-dihydropyrano[3,2-c]chromen-5-yl)acetamides II in good yields (80-95%) is reported. The 3-aryl-2-oxo-2,5-dihydropyrano[3,2-c]chromen-5-yl acetates III were prepared by cyclocondensation of 3-formylchromones (4-oxo-4H-chromene-3-carbaldehydes) and acetic acids in 64-86% yields. Acetamides II were obtained by reaction of 3-aryl-2-oxo-2,5-dihydropyrano[3,2-c]chromen-5-yl acetates III with AcNH2 catalyzed by p-TsOH in 80-93% yields. Click chem. precursors were prepared by propargylation of pyridones in 92-98% yields. They can serve for construction of more complex mols. possessing pyridone skeleton. Eleven novel compounds were screened for their anticancer activity on a panel of human tumor cell lines by NCI USA. These compounds selectively inhibit the growth of some of the tumor cell lines at 10-5 M (up to -33% compared to a control). The most sensitive tumor cell lines originated from kidney, breast, skin, ovary, blood and lung.
Chemical Papers published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Category: isoquinoline.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem