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Analogues 12′β-hydroxycephalostatin 1 ( 9 ), 7′-deoxyritterazine G ( 10 ), and 14- epi -7′-deoxyritterazine B ( 11 ) were prepared via our protocol for unsymmetrical pyrazine synthesis. Cytotoxicity against human tumors was also determined for the first time for ritterazines, with...
Simple mono-derivatisation of the aryl moiety of some phosphoramidate pronucleotide derivatives of d4A and ddA served to increase the lipophilicity of these membrane-soluble prodrugs. A concomitant and significant enhancement of potency against HIV-1 and HIV-2 in vitro was observed for the ddA-...
LB30057 ( 1 ) is a selective and efficacious oral thrombin inhibitor. Fluorine-substitution on the phenylene ring of the benzamidrazone portion in both compound 1 and its derivatives gave, in many cases, enhanced oral absorption in rats while maintaining the intrinsic potency and selectivity....
The C-acylation of Meldrum's acid by protected amino acids, using isopropenyl chloroformate (IPCF) as the condensing agent, is described. The process is used to synthesize γ and δ-amino-β-keto-esters.
The title compound, (−)-( S )- 9 , is a novel cardioselective calcium channel modulator that exhibits a calcium channel agonist effect on heart, a weak calcium channel antagonist effect on smooth muscle, and releases nitric oxide in vitro. (−)-( S )- 9 is a useful lead-compound for the design...
Synthetic dysidiolide, as well as several related compounds containing a γ-hydroxybutenolide moiety, were tested in in vitro Cdc25 assays against both synthetic and natural substrates. Contrary to literature values which are in the low micromolar range, we observe only millimolar inhibitory...
To investigate the phorbol ester-binding properties of the individual cysteine-rich motifs of protein kinase D (PKD), the 52-mer peptides containing each cysteine-rich motif of PKD (PKD-C1A, PKD-C1B) have been synthesized. The ( 3 H)phorbol-12,13-dibutyrate (PDBu) binding to PKD-C1A was affected...
Various optically pure benzocyclobutene and biphenylene-based α-amino acid derivatives are prepared in a very high diastereoselective manner via a six step sequence using Schöllkopf chiral auxiliary.
The synthesis of several-bioisosteric analogs based on the 3-OH-phenoxyethylamine dopamine D 2 agonist template (i.e., 3 ) is described. The benzimidazol-2-ones and benzthioimidazol-2-ones ( 7–10 ) and 2-trifluoromethyl-benzimidazole ( 13 ) were observed to have excellent affinity for the D 2...
Potent and selective thrombin inhibitors have been prepared with a piperazinedione template and L-amino acids. Likewise, incorporation of D-amino acids led to potent inhibitors with a novel mode of binding. Herein, the structure activity relationships and structural aspects of these compounds...
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