Synthesis and anti-microbial screening thiazoloquinazoline derivatives Abstract A series of some new 6,7,8,9-Tetrahydro-5H-5(2'-hydroxyphenyl)-2-(4'-fluorobenzylidine)-3-(4nitrophenyl amino) thiazolo quinazoline (4a-4d) and 6,7,8,9-Tetrahydro-5H-5-(2'-hydroxy phenyl)2-(4'-substituted benzylidine)-3-(4-nitrophenyl amino) thiazolo quinazoline (5a-5d) derivatives were synthesized. The in vitro ant...

Owing to the significant biological activities, quinazoline derivatives have drawn more and more attention in the synthesis and bioactivities research. This review summarizes the recent advances in the synthesis and biological activities investigations of quinazoline derivatives. According to the main method the authors adopted in their research design, those synthetic methods were divided into...

A series of 2,4-disubstituted quinazoline derivatives were designed and synthesized. The biological results showed that most of quinazoline derivatives exhibited potent antiproliferative activities against a panel of three tumor cell lines and a good inhibitory effect against the adhesion and migration of human umbilical vein endothelial cells (HUVECs). Among these compounds, 11d was the most p...

Re-investigation of the methanolic extract of Anisotes trisulcus (Forssk.) Nees aerial parts led to the isolation of two new tricyclic quinazoline alkaloids, 8-amino-7,8,9,11-tetrahydro-6H-pyrido[2,1-b]-quinazoline-2,6-diol (4) and 8-amino-3,6-dihydroxy-7,8,9-trihydro-6H-pyrido[2,1-b]quinazoline-11-one (5), and two quaternary ammonium compounds, (dimethylamino)-N-(hydroxymethyl)-N,N-dimethyl me...

A series of N(2),N(4)-disubstituted quinazoline-2,4-diamines has been synthesized and tested against Leishmania donovani and L. amazonensis intracellular amastigotes. A structure-activity and structure-property relationship study was conducted in part using the Topliss operational scheme to identify new lead compounds. This study led to the identification of quinazolines with EC50 values in the...

The original biologically active compound (BAS) N-[2-[4-oxo-3(4H)-quinazolinyl]propionyl]-guanidine (VMA-13-15), which has cardioprotective and neuroprotective activity, was synthesized on the basis of FSUE at VolgSMU Ministry Health Russian Federation. In accordance with XIV State Pharmacopoeia Federation, one criteria for quality control pharmaceutical substances is indicator "Related Impurit...

The asymmetric unit of the title compound, C15H12ClN3, contains two independent mol-ecules. The quinazoline ring system in each is essentially planar, with maximum deviations of 0.025 (16) and 0.0171 (16) Å. The dihedral angles between quinazoline ring systems and the phenyl rings are 88.25 (8) and 85.28 (16)° in the two independent mol-ecules. In the crystal, alternating independent mol-ecules...

Objective(s): We previously reported a series of quinazoline derivatives as vascular-targeting anticancer agents. In this study, we investigated the mechanism underlying the anti-angiogenic activity of the quinazoline derivative compound 11d. Materials and Methods: We examined the effects of quinazoline derivative 11d on vascular endothelial growth factor receptor-2 (VEGFR2) activation via VEG...

The chiral title compound, C(21)H(20)N(4)O(2), crystallizes as a racemic mixture. In the crystal, mol-ecules form centrosymmetric π-overlapping dimers [inter-planar distance = 3.338 (6) Å], which are further connected along the a axis forming centrosymmetric dimers via O-H⋯N hydrogen bonds. C-H⋯O inter-actions are also observed. The indolo[2,1-b]quinazoline group is somewhat bent, with a small ...

We have performed molecular docking on quinazoline antifolates complexed with human thymidylate synthase to gain insight into the structural preferences of these inhibitors. The study was conducted on a selected set of one hundred six compounds with variation in structure and activity. The structural analyses indicate that the coordinate bond interactions, the hydrogen bond interactions, the va...