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Synthesis of thienopyridine derivatives as potential antitumorals and/or antian...

Synthesis of new N-[3-(thieno[3,2-b]pyridine-7-ylthio)phenyl]benzamides as pote...

Angiogenesis, the growth of new vessels from preexisting vasculature, is a critical step in tumor progression [1]. The tyrosine kinase Vascular Endothelial Growth Factor Receptor 2 (VEGFR2) is a crucial mediator in angiogenesis since the VEGF, excreted by the tumor cells, binds to it activating several signaling pathways involved in cell survival and proliferation [2]. Recently thienopyridine derivatives showed...

Virtual screening of thieno[3,2-b]pyridine arylthioether (hetero)aryltriazole d...

Recently we presented a series of thieno[3,2-d]pyrimidinc ether I ,3-diaryl ureas with potent VEGFR2 inhibit ion activity. The binding mode was analyzed and the compounds showed a type-11 tyrosine kinase inhibition mode, with the thienopyrimidine moiety forming a Hydrogen Bond (H-bond) with CYS919 residue and the urea moiety forming a H-bonds with key residues G LU885 and ASP I 046 of the kinase domain. In thi...

Synthesis of 2-(hetero)arylthieno[2,3-b] or [3,2-b]pyridines from 2,3-dihalopyr...

A simple and efficient three-step methodology is described for the first time for the synthesis of 2-(hetero)arylthieno[2,3-b] or [3,2-b]pyridines. The first step is a Sonogashira coupling from 3-bromo-2-chloropyridine or 2-bromo-3-chloropyridine with several (hetero)arylalkynes to obtain the corresponding 2- or 3-chloro(hetero)arylethynylpyridines. These were cyclized by treatment with Na2S affording the exp...

Synthesis of 3-Halo-2-(Hetero)Arylthienopyridines through a three-step methodol...

Synthesis of the first thieno-delta-carboline : fluorescence studies in solutio...

The first thieno-delta-carboline (6,8,9-trimethyl-5H-pyrido[3,2-b]thieno[3,2-f]indole) was prepared in good yield (70%) by intramolecular palladium-assisted cyclization of an ortho-chlorodiarylamine. The latter was in turn selectively synthesized in high yield (90%) by C–N palladium catalyzed cross-coupling of 3-bromo-2-chloropyridine with, the also prepared, 6-amino-2,3,7- trimethylbenzo[b]thiophene. Fluoresce...

Evaluation of the antioxidant properties of diarylamines in the benzo[b]thiophe...

The antioxidant properties of substituted diarylamines in the benzo[b]thiophene series were evaluated by their reducing power and free radical scavenging activity. The results were compared with those of standards: acid ascorbic for the first method and BHA and BHT for the second. For both methods it was possible to establish some structure–activity relationships (SARs) based on the position of the arylaminatio...

Synthesis of the first thieno-δ-carboline. Fluorescence studies in solution and...

The first thieno-δ-carboline (6,8,9-trimethyl-5H-pyrido[3,2-b]thieno[3,2-f]indole) was prepared in good yield (70%) by intramolecular palladium-assisted cyclization of an ortho-chlorodiarylamine. The latter was in turn selectively synthesized in high yield (90%) by C–N palladiumcatalyzed cross-coupling of 3-bromo-2-chloropyridine with, the also prepared, 6-amino-2,3,7-trimethylbenzo[b]thiophene. Fluorescence st...

Palladium-catalysed amination of electron-deficient or relatively-rich benzo[b]...

Several diarylamines in the benzo[b]thiophene series were prepared by palladium catalyzed amination of ethyl 3-bromobenzo[b]thien-2-yl carboxylate with anilines and 5-aminoindole, in good to high yields using Pd(OAc)2, BINAP, Cs2CO3 in toluene. The presence of the ester group in the position 2 of the benzo[b]thiophene moiety increases the yields and lowers the heating times when compared with reactions using 3-...

Palladium-catalysed amination of electron-deficient or relatively electron-rich...

Several diarylamines in the benzo[b]thiophene series were prepared in good to high yields by palladium-catalysed amination of ethyl 3-bromobenzo[b]thiophene-2-carboxylate with anilines and 5-aminoindole in the presence of Pd(OAc)2, BINAP and Cs2CO3 in toluene. The presence of the ester group at the 2-position of the benzo[b]thiophene moiety increases the yields and lowers the heating times relative to the react...