86 research outputs found
Peptide and Peptide-Like Modulators of 20S Proteasome Enzymatic Activity in Cancer Cells
The involvement of the ubiquitinâproteasome pathway in the degradation of critical intracellular regulatory proteins suggested a few years ago the potential use of proteasome inhibitors as novel therapeutic agents being applicable in many different disease indications, and in particular for cancer therapy. This article reviews recent salient medicinal chemistry achievements in the design, synthesis, and biological characterization of both synthetic and natural peptide-like proteasome inhibitors, updating recent reviews on this class of agents. As shown herein, different compound classes are capable of modulating the subunit-specific proteolytic activities of the 20S proteasome in ways not previously possible, and one of them, bortezomib, has provided proof-of-concept for this therapeutic approach in cancer clinical settings
ChemInform Abstract: Aziridine Analogues of ((trans-(Epoxysuccinyl)-L-leucyl)amino)-4- guanidinobutane (E-64) as Inhibitors of Cysteine Proteases.
ChemInform Abstract: On Regioselectivity of Aldol Condensation of Aromatic Aldehydes with Borate Complex of Acetylacetone.
ChemInform Abstract: Probing the Specificity of the Serine Proteases Subtilisin Carlsberg and α-Chymotrypsin with Enantiomeric 1-Acetamido Boronic Acids. An Unexpected Reversal of the Normal âLâ-Stereoselectivity Preference.
A study of the donor properties of sialyl phosphites having an auxiliary 3-(S)-phenylseleno group
Synthesis of a Phosphonate Analog of Sialic Acid (Neu5Ac) Using Indium-Mediated Allylation of Unprotected Carbohydrates in Aqueous Media
Aziridine analogs of [[trans-(epoxysuccinyl)-L-leucyl]amino]-4-guanidinobutane (E-64) as inhibitors of cysteine proteases
NRC publication: Ye
On Regioselectivity of Aldol Condensation of Aromatic Aldehydes with Borate Complex of Acetylacetone
While cinnamoyl acetone 1 is obtained in good yield by a condensation of 3 molar excess of a borate complex of acetylacetone with benzaldehyde, products of Knoevenagel condensation 2 are predominantly obtained with furfural and 5-substituted furfurals. Cinnamoyl acetone 1 can be further condensed with furfural to form unsymmetrical curcuminoid 5. Compound 2a does not produce any new products under the same conditions. Compounds 3 and 5 are good inhibitors of growth of protozoan Trichomonas vaginalis
On Regioselectivity of Aldol Condensation of Aromatic Aldehydes with Borate Complex of Acetylacetone
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