Inosine 5'-monophosphate dehydrogenase (IMPDH) is one of the crucial enzymes in the de novo biosynthesis of guanosine nucleotides. It has served as an attractive target in immunosuppressive, anticancer, antiviral, and antiparasitic therapeutic strategies. In this study, pharmacophore mapping and molecular docking approaches were employed to discover novel Homo sapiens IMPDH (hIMPDH) inhibitors....

Various azido-ubiquinone derivatives were synthesized and characterized. 3-Azido-2-methyl-5-methoxy-6-(3,7-dimethyloctyl)-1,4-benzoquinone was found to be suitable for the study of specific interaction between ubiquinone (Q) and protein. It was synthesized with high specific radioactivity and used to identify the Q-binding proteins in purified ubiquinol-cytochrome c reductase. This azido-Q deri...

Pharmacophore development, 3D-QSAR and docking studies were performed on twenty eight pyrrolotriazine derivatives as Aurora A kinase inhibitors. Five point pharmacophores with one hydrogen bond acceptor (A2), two hydrogen bond donor (D8, D11), one positive ionic (P15) and one aromatic ring (R17) as pharmacophoric features were developed. Amongst them the Pharmacophore hypothesis ADDPR.55 yielde...

Unnatural sugar-mediated metabolic labeling of cancer cells, coupled with efficient Click chemistry, has shown great potential for in vivo imaging and cancer targeting. Thus far, chemical labeling of cancer cells has been limited to the small-sized azido groups, with the large-sized and highly hydrophobic dibenzocyclooctyne (DBCO) being correspondingly used as the targeting ligand. However, sur...

Introduction During an evaluation of azido-α-amino acids and their utility in solid-phase peptide chemistry, the octapeptide angiotensin II and a tripeptide thyrotropin-releasing hormone (TRH) analog have been prepared using Meldal’s procedure [1]. A necessary novel step was the reduction of the azido moiety of L-proline, a secondary amine constrained by a ring, to the corresponding free amine ...

Within this work, a modified preparation of diethyl 4-azidobenzylphosphonate (L1) is presented and the family 4- or 4′-azido-substituted aromatic phosphonate esters increased by three new ligand platforms: diisopropyl (L2), ((4′-azido-[1,1′-biphenyl]-4-yl)methyl)phosphonate (L3), 4-azido-2,3,5,6-tetrafluorobenzylphosphonate (L4), which exhibit an anomalous splitting N3 stretching vibrations. Su...

The Staudinger ligation between an azido-protein and a phosphinothioester-derivatized surface is demonstrated to be an effective means for the site-specific, covalent immobilization of a protein. Immobilization yields of >50% are obtained in <1 min, and immobilized proteins have >80% of their expected activity. No other method enables more rapid immobilization or a higher yield of active protei...

Two light-sensitive analogs of 2,4-dichlorophenoxyacetic acid, namely 4-azido-2-chlorophenoxyacetic acid and 3-azido-5-chlorophenoxyacetic acid, have been synthesized for use as auxin photoaffinity labels. The preparation and biological activity of the compounds are described. Both contain the photolabile azido group; the 2,4-substituted compound shows auxin activity and the 3,5-substituted com...

The aggregating effect of ADP on human platelets and the inhibiting effect of adenosine are apparently mediated by different receptors on the cells’ outer membranes. Photolysable azido-analogues of adenosine, AMP and ADP have been prepared so tha t the receptors for them can be labelled. 2-Azidoadenosine inhibited platelet aggregation by ADP more than adenosine itself and increased platelet cAM...

A novel type of zwitterionic HILIC stationary phase was prepared by covalently bonding the l-azido lysine on silica gel via click chemistry. The key intermediate azido lysine was synthesized by transformation the amino group in l-Boc-lysine to corresponding azido group and subsequent removal of the N-protected group (Boc). Finally, the azido lysine was covalently bonded to silica beads by click...