60853-81-8Relevant academic research and scientific papers
Amino pyrimidine compound and preparation method and application thereof
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Paragraph 0437; 0440; 0441; 0442, (2018/11/22)
The invention relates to an amino pyrimidine compound and a preparation method and application thereof. The amino pyrimidine compound has a structure as shown in a formula I. The formula is shown in the description. The compound is an inhibitor of an epidermal growth factor receptor (EGFR) kinase. The invention further relates to a medicine composition comprising the compound, a preparation methodand application thereof in preparation of anti-tumor medicines.
Development of a series of bis-triazoles as G-quadruplex ligands
Saleh, Maysaa M.,Laughton, Charles A.,Bradshaw, Tracey D.,Moody, Christopher J.
, p. 47297 - 47308 (2017/10/19)
Maintenance of telomeres-specialized complexes that protect the ends of chromosomes-is provided by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but absent in most normal cells. Targeting telomere maintenance mechanisms could potentially halt tumour growth across a broad spectrum of cancer types. Telomeric ends of chromosomes consist of noncoding repeat sequences of guanine-rich DNA. These G-rich ends can fold into structures called G-quadruplexes. Stabilization of G-quadruplexes by small binding molecules called G4 ligands can prevent telomerase enzyme from maintaining telomere integrity in cancer cells. G-quadruplexes can exist in other parts of the genome too, especially within promoter sequences of oncogenes, and also be interesting drug targets. Here, we describe the development of a new series of novel bis-triazoles, designed to stabilize G-quadruplex structures selectively as G4 ligands. FRET assays showed two compounds to be moderately effective G4 binders, with particular affinity for the quadruplex formed by the Hsp90a promoter sequence, and good selectivity for G-quadruplex DNA vs. duplex DNA. However, CD spectroscopy failed to provide any information about the folding topology of the human telomeric G-quadruplex resulting from its interaction with one of the ligands. All the new ligands showed potent cell growth inhibitory properties against human colon and pancreatic cancer cell lines, as evidenced by the MTT assay; notably, they were more potent against cancer cells than in fetal lung fibroblasts. Docking studies were performed to rationalize the affinity of these ligands for binding to the telomeric parallel G-quadruplex DNA.
Binding enhancements of nicotinic acid to water-soluble zinc porphyrins based on triple attractions of coordination, Coulomb, and CH-π interactions
Imai, Hiroyasu,Munakata, Hiroki,Uemori, Yoshio
experimental part, p. 969 - 972 (2009/08/15)
The binding of amines to artificial zinc-porphyrin receptors 1-4 was examined in basic aqueous solutions. For nicotinic acid and 3,5- dicarboxypyridine, substantial binding enhancements were observed compared to other amines with no π system or carboxyl group. This observation suggested that interligand attractions of Coulomb and CH-π interactions in addition to N-atom coordination can act effectively as recognition factors. The differences in the Coulomb interaction between carboxylate and sulfonate anions were also discussed.
Prodrugs of imidazopyridine derivatives
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, (2008/06/13)
Compounds of formula (1), in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.
HETEROCYCLIC MODULATORS OF NUCLEAR RECEPTORS
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, (2008/06/13)
Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.
Glycylcyclines. 1. A New Generation of Potent Antibacterial Agents through Modification of 9-Aminotetracyclines
Sum, Phaik-Eng,Lee, Ving J.,Testa, Raymond T.,Hlavka, Joseph J.,Ellestad, George A.,et al.
, p. 184 - 188 (2007/10/02)
This report describes the discovery of a new generation of tetracycline antibacterial agents, the "glycylcyclines".These agents are notable for their activity against a broad spectrum of tetracycline-susceptible and -resistant Gram-negative and Gram-positive aerobic and anaerobic bacteria possessing various classes of tetracycline-resistant determinants .The design and synthesis of a number of 7-substituted 9-substituted-amido 6-demethyl-6-deoxytetracyclines are described.
