80621-90-5Relevant articles and documents
PRODRUG DERIVATIVES OF SUBSTITUTED TRIAZOLOPYRIDINES
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Page/Page column 136; 137, (2015/01/09)
The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.
Preparation of asymmetric urea derivatives that target prostate-specific membrane antigen for SPECT imaging
Harada, Naoya,Kimura, Hiroyuki,Ono, Masahiro,Saji, Hideo
, p. 7890 - 7901 (2013/11/06)
Prostate-specific membrane antigen (PSMA) has been identified as a diagnostic and therapeutic target for prostate cancer. (S)-2-[3-[(R)-1-Carboxy- 2-mercaptoethyl]ureido-pentanedioic acid (Cys-CO-Glu) were used to design novel PSMA targeting probes by nucleophilic conjugate addition between cysteine and maleimide based reagents. 3 ([123I]IGLCE) was synthesized by this strategy and showed high affinity for PSMA. Results of binding inhibition assays of these derivatives suggested the importance of an aromatic group and succinimide moiety for high affinity. [123I]3 was evaluated in vivo with PSMA positive LNCaP and PSMA negative PC-3 human prostate cancer xenograft bearing mice. [125I]3 accumulated in LNCaP tumors but not in PC-3 tumors, and the accumulation was inhibited by 2-(phosphonomethyl)pentanedioic acid (2-PMPA). Use of [123I]3 provided positive images of LNCaP tumors in single photon emission tomography scans. These results warrant further evaluation of [123I]3 and its derivatives as radiolabeled probes for the diagnosis of prostate cancer.
CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY AND PROCESSES FOR THEIR PREPARATION
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Page/Page column 75-76, (2008/06/13)
The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administ
Evaluation of chelating agents as anti-angiogenic therapy through copper chelation
Camphausen, Kevin,Sproull, Mary,Tantama, Steve,Venditto, Vincent,Sankineni, Sandeep,Scott, Tamalee,Brechbiel, Martin W.
, p. 5133 - 5140 (2007/10/03)
A set of novel polyamine hexadentate cis,cis-1,3,5,-triaminocyclohexane (tach) chelating agents were synthesized and evaluated in conjunction with a selection of both linear and macrocyclic polyamines as copper chelators for novel anti-angiogenic therapy in an in vitro endothelial cell proliferation assay to assess their cytotoxicity and selectivity. Macrocyclic polyamine 15 exhibited the greatest selective activity in this assay while the tach based ligands exhibited cytotoxicity, but no selectivity. The evaluation of several sets of polyamine donor chelating agents including a selection of novel hexadentate 1,3,5-cis,cis-triaminocyclohexane (tach) based derivatives were performed in an in vitro endothelial cell proliferation assay to assess their cytotoxicity and selectivity as novel anti-angiogenic agents. The selective nature of the anti-angiogenic agents for human umbilical vein endothelial cells (HUVEC) was compared to a normal fibroblast cell line and a human Glioma cell line to evaluate these compounds. Linear tri- and tetra-polyamines were superior to both macrocyclic and the tach based polyamine chelating agents in terms of selectivity of its inhibitory activity toward the proliferation of HUVEC cells compared to the fibroblast and human Glioma cells. The linear polyamine, triethylenetetramine (22), previously reported to possess anti-angiogenic properties failed to demonstrate any selectivity for inhibiting the proliferation of HUVEC cells compared to the fibroblast and human Glioma cells.
Synthesis of N-urethane-protected γ-amino-functionalized butenoates and tautomeric studies by means of NMR, X-ray crystallography and ab initio calculations
Detsi, Anastasia,Gavrielatos, Efstathios,Adam, Marion-Alexandra,Igglessi-Markopoulou, Olga,Markopoulos, John,Theologitis, Marcos,Reis, Heribert,Papadopoulos, Manthos
, p. 4337 - 4342 (2007/10/03)
N-Urethane-protected γ-amino-α-cyano-β-hydroxybutenoates were synthesized as potential statine analogues and the stability of their possible tautomers was assessed using NMR, X-ray crystallography and ab initio calculations. The results establish that the cis-enol tautomeric form is the most stable one both in solution (CDCl3) and in the solid phase. In full agreement with the experimental data, the theoretical calculations predicted that the cis-enol tautomer would be the minimum energy tautomer.
Synthesis and radioprotective activity of new N-(amino acid)-S-acetylcysteamine and cystamine derivatives
Oiry,Pue,Fatome,Sentenac-Roumanou,Lion,Imbach
, p. 809 - 817 (2007/10/02)
In order to evaluate the influence of an amino acid conjugation (Sar,Ser, Phe, Pro, Thz) on S-acetylcysteamine, cystamine, N-(amino acid)-S-acetylcysteamine (14-18) and N,N'-bis (amino acid) cystamine (24-28) derivatives have been synthesized and evaluated as potential radioprotectors. Their toxicity and radioprotective activity, as the dose reduction factor (DRF) have been determined (in vivo; ip) and compared with cysteamine and cystamine parent compounds: N-glycyl-S-acetylcysteamine trifluoroacetate 1 and N,N'-bis (glycyl)cystamine bis (trifluoroacetate) 2. Among these compounds, 14 (Sar), 15 (Ser), 15a [Ser (Ac)], 16 [Phe], 24 (Sar) had significant radioprotective activity.