MAP Kinase Interacting Serine/Threonine Kinase 1 (MNK1) play important roles in the signaling transduction of MAPK pathways. It is significantly overexpressed in renal clear cell carcinoma and head-neck squamous cell carcinoma tissues in both mRNA and protein levels. Based on the crystallographi...

A total of 66 novel heterofused pyrimidine analogues (pyrazolo[3,4-d]pyrimidine (7-43) and pyrido[2,3-d]pyrimidine (51a-l & 52a-h)) were synthesized by employing suitable methods. The desired structures of all the synthesized compounds were confirmed based on FT-IR, 1H NMR, 13C NMR and HRMS expe...

Novel candidates of thiazolo[4,5-d]pyrimidines (9a-l) were synthesized and their structures were elucidated by spectral and elemental analyses. All the novel derivatives were screened for their cyclooxygenase inhibitory effect, anti-inflammatory activity and ulcerogenic liability. All the new co...

Chiral poly(glycerol methacrylate)s (PGMAs) are synthesized via ATRP using enantiopure solketal methacrylates followed by acidic hydrolysis. The optical activity of the polymers is confirmed by measurements of the circular dichroism. Furthermore, the chirality of the PGMAs containing repeat unit...

Dielectric and mechanical relaxation processes in the series of poly(n-alkyl methacrylates) (PnAMA) depend systematically on the number of carbons in the alkyl part of the side chain. The crossover region of the dynamic glass transition shifts to lower frequencies for increasing this C number an...

As a test as to whether the title intermediate 13 can be liberated from 3-bromo-1,2-dihydronaphthalene (19), the latter was treated with potassium tert-butoxide (KOtBu). Being the major products, naphthalene (20) and 3-tert-butoxy-1,2-dihydronaphthalene (21) provide unambiguous evidence for the ...

A series of 2,4-diarylaminopyrimidine derivatives containing dithiocarbamate moiety were designed by molecular hybridization strategy and synthesized for screening as inhibitors of focal adhesion kinase (FAK). Most of these compounds exhibit significant antiproliferative activities on human canc...

A series of prostaglandin DP agonists containing a 3-oxa-15-cyclohexyl motif was synthesized and evaluated in several in vitro and in vivo biological assays. The reference compound ZK 118.182 (9β-chloro-15-cyclohexyl-3-oxa-ω-pentanor PGF2α) is a potent full agonist at the prostaglandin DP rec...

Enantiopure [(2S,4R)-1-cyclohexyl-4-methylpiperidin-2-yl]methanol 5a and [(2S,4R)-1-cyclohexyl-4-methylpiperidin-2-yl]-(diphenyl)methanol 5b, new β-amino alcohols based on l-pipecolinic acid (homoproline), have been prepared straightforwardly from rac-alaninol and rac-2-amino-1,1-diphenylpropan...

α-hydroxy statine 5 was synthesized by osmylation of amido crotonate 6 and incorporated into peptide framework 9, resulting in an active renin inhibitor; predicted stereochemical preferences for renin inhibition were confirmed by x-ray analysis and biochemical determinations. The facial selecti...

A new strategy for enantioselective assembly of the trisubstituted tetrahydrofuran ring has been established for synthesis of the C1–C12 acid fragment of amphidinolide T series marine macrolides. The key steps involve the SmI2-mediated highly enantioselective reductive coupling of an aldehyde w...

Ethyl, n-propyl, iso-propyl and n-butyl crotonates were polymerized by group transfer polymerization (GTP) using ketene trialkylsilyl acetals as initiators in the presence of mercury (II) iodide as catalyst and iodotriethylsilane as co-catalyst. Predominantly disyndiotactic polymers with number-...

Aspergillus oryzae, isolated from traditional Japanese food “Miso”, has efficiently catalyzed the direct esterification between acetic acid and cis-3-hexen-1-ol in organic solvent. The esterification between acids and alcohols having different chain lengths was initially investigated, observin...

A series of N,N-3-phenyl-3-benzylaminopropanamide derivatives were identified as novel CETP (cholesteryl ester transfer protein) inhibitors. In our previous study, lead compound L10 was discovered by pharmacophore-based virtual screening (Dong-Mei Zhao et al., 2014). Based on L10 (IC50 8.06 μM)...

A group of novel l-serinamides, substituted (S)-2-(benzylideneamino)-3-hydroxy-N-tetradecylpropanamides (3a–o) and substituted (S)-2-(benzylamino)-3-hydroxy-N-tetradecyl propanamides (4c, 4i, 4l, and 4o), were synthesized as potential anti-tumor lead compounds. In vitro cell viability assay res...

Structure–activity relationships for the A-region in a series of N-4-t-butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamides as TRPV1 antagonists have been investigated. Among them, the 3-fluoro analogue 54 showed high binding affinity and potent antagonism for both rTRPV1 and hTRPV1 in CHO ...

1,3-Dipolar cycloadditions of 2-thio-3-chloroacrylamides with nitrile oxides and nitrones is described. A series of novel isoxazolines are isolated from the nitrile oxide cycloadditions, whilst the isoxazolines generated from the nitrone cycloadditions undergo further ring opening to yield piper...

Diastereoselective sulfur oxidation in 2-thio-3-chloroacrylamides is described. A range of chiral amine auxiliaries was incorporated in the β-chloroacrylamide, and the efficiency with which the stereochemistry was relayed to the sulfur centre during sulfoxidation was investigated. Diastereomeri...

A highly enantioselective synthesis of Pregabalin 1 hydrochloride with good overall yield (44%) and enantioselectivity (98% ee) was described. The key step is an asymmetric Michael addition of equivalent of diethyl malonate and nitroalkene under solvent-free conditions using thiourea 2 as cataly...

The Schiff base compound, 5-(diethylamino)-2-((3-nitrophenylimino)methyl)phenol, C17H19O3N3, was synthesized and characterized by IR, UV–Vis and single-crystal X-ray diffraction (XRD) technique. The title compound prefers enol tautomeric form in solid state as to X-ray, IR and UV–Vis spectra r...