The Front Cover shows 5-bromo-2-(tetrahydro-2H-pyran-4-yl)pyridine – one of many sp3-enriched pyridine derivatives prepared on a multigram scale by group Ukrainian chemists. background photo Anatolii Varenyk depicts the Kilometre Zero Ukraine Sign (also known as “The Winged Globe”) control point located Independence Square (Maidan Nezalezhnosti) in Kyїv. More information can be found Research A...

silica-bonded n-propyltriethylene-tetramine (sbnptt) was found as an efficient solid base for the synthesis of 2-amino-5-oxo-5,6,7,8-tetrahydro-4h-chromenes. chromene derivatives were obtained via the three-component condensation reaction of aromatic aldehydes, malononitrile, and dimedone at 80 oc under solvent-free conditions. the heterogeneous solid base showed much the same efficiency when u...

Two series of fused tetrahydro-β-carboline hydantoin and tetrahydro-β-carboline thiohydantoin derivatives with a pendant 2,4-dimethoxyphenyl at position 5 were synthesized, and chiral carbons at positions 5 and 11a swing from R,R to R,S, S,R, and S,S. The prepared analogues were evaluated for their capacity to inhibit phosphodiesterase 5 (PDE5) isozyme. The R absolute configuration of C-5 in th...

A new series of tetrahydro-quinazoline and tetrahydro-1H-dibenzo[b,e][1,4]diazepine analogs were synthesized and tested for their DHFR inhibition and in vitro antitumor activity. Compound 35 showed a remarkable DHFR inhibitory potency (IC₅₀, 0.004 μM) which is twenty fold more active than methotrexate (MTX). Compounds 17 and 23 proved to be fifteen fold more active than the known antitumor 5-FU...

Although all-oral direct-acting antiviral (DAA) therapy for hepatitis C virus (HCV) treatment is now a reality, today's HCV drugs are expensive, and more affordable drugs are still urgently needed. In this work, we report the identification of the 2-phenyl-4,5,6,7-Tetrahydro-1H-indole chemical scaffold that inhibits cellular replication of HCV genotype 1b and 2a subgenomic replicons. The anti-H...

The crystal structures of 4-(4-methylphenyl)-6-phenyl-2,3,3a,4-tetrahydro-1H-pyrido[3,2,1-jk]carbazole (IIa) and 4-(4-methoxyphenyl)-6-phenyl-2,3,3a,4-tetrahydro-1H-pyrido[3,2,1-jk]carbazole (IIb) were elucidated by single crystal X-ray diffraction. Compound (IIa), C28H25N, crystallizes in the triclinic system, space group P-1, with a = 8.936(2) Å, b = 10.490(1) Å, c = 11.801(1) Å, α = 102.69(5...

Tetrahydro-iso-alpha acids commonly called THIAA or Tetra are modified hop acids extracted from hop (Humulus lupulus L.) which are frequently used in brewing industry mainly in order to provide beer bitterness and foam stability. Interestingly, molecular structure of tetrahydro-iso-alpha acids is close to a new type of estrogen receptor alpha (ERα) antagonists aimed at disrupting the binding of...

Silica-bonded n-propyltriethylene-tetramine (SBNPTT) was found as an efficient solid base for the synthesis of 2-amino-5-oxo-5,6,7,8-tetrahydro-4H-chromenes. Chromene derivatives were obtained via the three-component condensation reaction of aromatic aldehydes, malononitrile, and dimedone at 80 oC under solvent-free conditions. The heterogeneous solid base showed much the same efficiency when u...

The cyclization of b-anilino propionic acids in the presence of polyphosphoric acid (PPA) afforded the 2,3-Dihydroquinoline-4-(1H)-ones in good yields. N,N'-bis(2-carboxyethyl)-4-methyl-1,2-diaminobenzene (7) is cyclized under this condition to produce the 1,5-diaza-2,3,6,7-tetrahydro-4-methyl-pheranthrene-4,8-dione(bis-quinolone) (8).