A series of amino acid ester derivatives containing 5-fluorouracil were synthesized using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC*HCl) and N-hydroxybenzotriazole (HOBt) as a coupling agent. The structures of the products were assigned by NMR, MS, IR etc. The in vitro antitumor activity tests against leukaemia HL-60 and liver cancer BEL-7402 indicated that (R)-ethyl 2-(2...

ABSTRACT : Dihydropyrimidines (DHPMs) are of much importance due to excellent pharmacological properties. In this account we have synthesized new functionalized DHPMs (a) 5-benzoyl-6-methyl-4-phenyl-3,4dihydropyrimidin-2(1H)-one (KT-01) and (b) 5-benzoyl-4-(4-chlorophenyl)-6-methyl-3,4-dihydropyrimidin-2(1H)-one (KT-03) in two step reaction. The first step involves the synthesis of benzoylaceto...

UNLABELLED Ruthenium (Ru) complexes are currently the focus of substantial interest because of their potential application as chemotherapeutic agents with broad anticancer activities. This study investigated the in vitro and in vivo anticancer activities and mechanisms of two Ru complexes-2,3,7,8,12,13,17,18-Octaethyl-21H,23H-porphine Ru(II) carbonyl (Ru1) and 5,10,15,20-Tetraphenyl-21H,23H-por...

Interactions of porphyrin derivatives 5,10,15,20-tetrakis(N-methylpyridinium-4-yl)-21H,23Hporphyrin (TMPyP4) and 5,10,15,20-tetrakis(N-propylpyridinium-4-yl)-21H,23H-porphyrin (TPrPyP4) with human telomeric AG3(T2AG3)3 G-quadruplex DNAs in 150 mM K -containing buffer in the presence or absence of 40% molecular crowding agent poly(ethylene glycol) (PEG 200) were studied by absorption titration f...

A convenient and highly efficient procedure for the synthesis of 3,4-dihydropyrimidin-2-(1H)-one/thione derivatives via one-pot three-component Biginelli condensation of arylaldehydes,urea/thiourea and ethyl/methyl acetoacetate in the presence of Zn(SO4)2.7H2Oas anefficient, readily and inexpensive catalyst under solvent-free conditions have been studied. Thisprotocol ha...

Dasabuvir [also known as ABT-333 or N-(6-(3-(tert-butyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methoxyphenyl)naphthalen-2-yl)methanesulfonamide] is a potent non-nucleoside NS protein 5B polymerase inhibitor of the hepatitis C virus (HCV) and is being developed in combination with paritaprevir/ritonavir and ombitasvir in an oral regimen with three direct-acting antivirals for the treatme...

The reaction of 3-cyclohexyl-2-(cyclohexylimino)-6-(4-ethoxyphenyl)-5-(4-methyl-3-oxo-3,4-dihydroquinoxalin-2-yl)-2,3-dihydro-4H-1,3-oxazin-4-one with ammonium acetate afforded 3-(1-cyclohexyl-2-(cyclohexylamino)-4-(4-ethoxyphenyl)-6-oxo-1,6-dihydropyrimidin-5-yl)-1-methylquinoxalin-2(1H)-one in a good yield. compound was fully characterized.