The in silico identification, optimization and crystallographic characterization of a 6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]isoquinolin-1-amine scaffold as an inhibitor for the EPHA4 receptor tyrosine kinase is described. A database containing commercially available compounds was subjected to an in silico screening procedure which was focused on finding novel, EPHA4 hinge binding fragments. This...

We have developed a new technology called multi-catalysis for the sequential one-pot synthesis of highly functionalized heterocycles. A practical and novel multi-component aniline-, self- and Brønsted acid-catalyzed selective process for the sequential one-pot synthesis of highly substituted 2-(2-hydroxy-aryl)-cyclopentane-1,3-diones, 3,9-dihydro-2H-cyclopenta[b]chromen-1-ones and 3,3-dimethyl-...

The title compounds, C22H22N4 and C24H26N4O2 [alternative names: 2,6-dibenzyl-2,3,6,7-tetrahydro-1H,5H-dipyrrolo[3,4-b; 3',4'-e]pyrazine and 2,6-bis(4-methoxybenzyl)-2,3,6,7-tetrahydro-1H,5H-dipyrolo[3,4-b;3',4'-e]pyrazine], two 1,2,3,5,6,7-hexahydro-2,4,6,8-tetraaza-s-indacene derivatives, are both centrosymmetric and have similar S-shaped structures. In the former, there are two independent m...

Epingaione (4-Methyl-1-(5-methyl-2, 3,4,5-tetrahydro-[2,3']bifuranyl-5-yl)-pentan-2-one) was isolated as one of the major lipophilic secondary metabolites from the leaves and stems of Bontia daphnoides L. The compound gave 79.24% and 50.83% anti-proliferation/cytotoxic activity on the human SH-SY5Y neuroblastoma and TE-671 sarcoma cells in vitro at 50 pg/mL, respectively. Epingaione was transfo...

The method of electrophilic intramolecular cyclization is widely used for the synthesis condensed thienopyrimidine derivatives. In this work, regioselectivity process terminally substituted allylic derivatives, but-1-enyl and propargyl thioethers with p-methoxyphenyltellurttrichloride was investigated.
 It established that as a result tellurium-induced butenyl 5,6-dimethyl-3-phenylthieno[2...

The NCNN group is an essential part of various heterocycles bearing high biological activities. 1,2,4-Triazines and their condensed derivatives found applications as pharmaceuticals and in agriculture. For example vardenafil ñ phosphodiesterase inhibitor, is useful in the treatment of male erectile dysfunctions (1), apazone exhibit anti-inflammatory and analgesic actions (2), lamotrigine is use...

cobalt hydrogensulfate is an efficient catalyst for the condensation of β-naphthol, aromatic aldehydes and 5,5-dimethyl-1,3-cyclohexanedione at 120 °c to afford 9,9-dimethyl-12-phenyl-8,10,11,12-tetrahydro-9-h-benzo[a]xanthen-11-one derivatives in high yields. also, polycondensation reactions of phenols with phthalic anhydride were carried out in the presence of cobalt hydrogensulphate under so...