Biologically as well medicinally important two different organic scaffolds, viz. benzimidazole and quinazoline, are present in the class of heterocyclic compounds called benzimidazoquinazolinone. Similarly, indolylxanthenones containing moieties such indole xanthene. In this work, a new green protocol for synthesis benzoimidazoquinazolinone indolylxanthenone derivatives was attained under envir...

Irreversible EGFR inhibitors can circumvent acquired resistance to first-generation reversible, ATP-competitive inhibitors in the treatment of non-small-cell lung cancer. They contain both a driver group, which assures target recognition, and a warhead, generally an acrylamide or propargylamide fragment that binds covalently to Cys797 within the kinase domain of EGFR. We performed a systematic ...

A series of novel ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acids 2a-d and esters 3a-l were synthesized and evaluated for antimicrobial activity. Alkylation of potassium 2-thio-[1,2,4]triazolo[1,5-c]quinazoline 1 with halogenocarboxylic acids and its esters proceeded S-regioselectively. During acid catalyzed esterification of 2a-c, degradation of the pyrimidine ring was observed. Th...

Purpose: To synthesize a new series of 1-substituted-4-(pyridin-4-yl) [1,2,4] triazolo[4,3-a]quinazolin5(4H)-ones and evaluate them for H1-antihistaminic activity with negligible side effects in guinea pigs. Methods: The synthesized compounds were characterized by Infrared spectroscopy (IR), proton nuclear magnetic resonance (H-NMR) and mass spectrometry (MS) data. The purity of the compounds w...

A new porphyrin-based porous organic polymer (POP) with BET surface area ranging from 780 to 880 m(2)/g was synthesized in free-base form via the reaction of meso-tetrakis(pentafluorophenyl) porphyrin and a rigid trigonal building block, hexahydroxytriphenylene. The material was then metallated with Fe(III) imparting activity for Lewis acid catalysis (regioselective methanolysis ring-opening of...

A new series of 2-[2-(2,6-dichlorophenyl)amino]phenyl methyl -3-[(1-phenyl-5-substituted phenyl)-5-hydro-1H-pyrazol-3-yl-amino]-6,8-dibromoquinazolin-4(3H)-ones C1-13 have been synthesized by the reaction of 2-[2-(2,6-dichlorophenyl)amino]phenylmethyl-3-substituted phenyl chromene amido-6,8-dibromo-quinazolin-4(3H)-ones with phenylhydrazine in the presence of glacial acetic acid. The chalcones ...

Three new alkaloids, including auranomides A and B (1 and 2), a new scaffold containing quinazolin-4-one substituted with a pyrrolidin-2-iminium moiety, and auranomide C (3), as well as two known metabolites auranthine (4) and aurantiomides C (5) were isolated from the marine-derived fungus Penicillium aurantiogriseum. The chemical structures of compounds 1-3 were elucidated by extensive spectr...

A library of thirty eight novel thiazolo[5,4-f]quinazolin-9(8H)-one derivatives (series 8, 10, 14 and 17) was prepared via the Hügershoff reaction and a Cu catalyzed intramolecular C-S bond formation, helped by microwave-assisted technology when required. The efficient multistep synthesis of the key 6-amino-3-cyclopropylquinazolin-4(3H)-one (3) has been reinvestigated and performed on a multigr...