282524-97-4Relevant academic research and scientific papers
Emerging Anticancer Activity of Candidal Glucoseamine-6-Phosphate Synthase Inhibitors upon Nanoparticle-Mediated Delivery
Kertmen, Ahmet,Przysiecka, Lucja,Coy, Emerson,Popenda, Lukasz,Andruszkiewicz, Ryszard,Jurga, Stefan,Milewski, Slawomir
, p. 5281 - 5293 (2019)
Numerous glutamine analogues have been reported as irreversible inhibitors of the glucosamine-6-phosphate (GlcN-6-P) synthase in pathogenic Candida albicans in the last 3.5 decades. Among the reported inhibitors, the most effective N3-(4-methox
NOVEL ARYL-CYANOGUANIDINE COMPOUNDS
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Page/Page column 76; 78, (2016/10/31)
The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine- pyrazolines of general formula (I), wherein R1, R2, R3, R4 and R5 have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyperproliferative disorders, in particular for cancer, respectively tumour disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.
Solid-phase synthesis of 6,7-cycloalkane-fused 1,4-diazepane-2,5-diones via a cyclization/release strategy
Caroen, Jurgen,Clemmen, An,Kámán, Judit,Backaert, Fréderique,Goeman, Jan L.,Fül?p, Ferenc,Van Der Eycken, Johan
, p. 148 - 160 (2015/12/23)
A solid-phase synthesis procedure for the parallel preparation of 6,7-cycloalkane-fused 1,4-diazepane-2,5-diones is described. The methodology applies α- and alicyclic β-amino acid building blocks to construct the seven-membered heterocyclic core, while a
Hairpin folding behavior of mixed α/β-peptides in aqueous solution
Lengyel, George A.,Frank, Rebecca C.,Horne, W. Seth
, p. 4246 - 4249 (2011/06/21)
The invention of new strategies for the design of protein-mimetic oligomers that manifest the folding encoded in natural amino acid sequences is a significant challenge. In contrast to the α-helix, mimicry of protein β-sheets is less understood. We report
Synthesis and properties of novel pyrrolidinyl PNA carrying β-amino acid spacers
Vilaivan, Tirayut,Suparpprom, Chaturong,Harnyuttanakorn, Pongchai,Lowe, Gordon
, p. 5533 - 5536 (2007/10/03)
Novel pyrrolidinyl peptide nucleic acids comprising alternate sequences of nucleobase-modified d-proline and β-amino acid spacers selected from L-aminopyrrolidine-2-carboxylic acid, D-aminopyrrolidine-2-carboxylic acid, (1R,2S)-2-aminocyclopentane carboxylic acid and β-alanine were synthesized using solid phase methodology. Gel-binding shift assay revealed that only the homothymine PNA decamer bearing D-aminopyrrolidine-2-carboxylic acid spacer binds with (dA)10.
Large-scale syntheses of FMOC-protected non-proteogenic amino acids: Useful building blocks for combinatorial libraries
Dener, Jeffrey M.,Fantauzzi, Pascal P.,Kshirsagar, Tushar A.,Kelly, Daphne E.,Wolfe, Aaron B.
, p. 445 - 449 (2013/09/07)
Convenient and reliable large-scale procedures for the protection of various amino acids with N-(9-fluorenylmethoxycarbonyl)oxysuccinimide (FMOC-OSu) are described. Commercially available 4-aminomethylbenzoic acid and trans-4-(aminomethyl)cyclohexanecarbo
