192643-84-8Relevant articles and documents
ECTONUCLEOTIDE PYROPHOSPHATASE/PHOSPHODIESTERASE 1 (ENPP1) MODULATORS AND USES THEREOF
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Paragraph 00606; 00612, (2021/07/02)
Provided herein are small molecule modulators of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS, METHODS OF MAKING, AND METHODS OF USE THEREOF
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Page/Page column 82, (2019/12/25)
Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutica
New 13-pyridinealkyl berberine analogues intercalate to DNA and induce apoptosis in HepG2 and MCF-7 cells through ROS mediated p53 dependent pathway: Biophysical, biochemical and molecular modeling studies
Chatterjee, Sabyasachi,Mallick, Sumana,Buzzetti, Franco,Fiorillo, Gaetano,Syeda, Tanjia Monir,Lombardi, Paolo,Saha, Krishna Das,Kumar, Gopinatha Suresh
, p. 90632 - 90644 (2015/11/11)
A new series of 13-pyridinealkyl berberine analogues was synthesized and their DNA binding efficacy studied by employing spectroscopic, calorimetric and molecular modeling techniques. Analogues with more than one CH2 group showed better intercalative binding than berberine. The analogue with one CH2 group bound DNA weaker than berberine. The binding of the analogue with single CH2 group was entropy driven, while those with more than one CH2 group was favoured by both entropy and enthalpy changes. Higher salt concentration and temperature destabilized the binding. A larger contribution from non-polyelectrolytic forces to the Gibbs energy and the involvement of strong hydrophobic interactions were inferred. Molecular modeling pin pointed the specific binding site and the non-covalent interactions in the association. The best DNA binding analogue (BER5) inhibited the growth of hepatocellular and breast carcinoma most efficiently. It induced apoptosis in HepG2 and MCF-7 cells with externalization of phosphatidylserine and reactive oxygen species generation with accumulation of cells in the G0/G1 phase. Furthermore, up regulation of p53 and p21 indicated the role of p53 in BER5 mediated apoptosis. The results suggested that 13-pyridinealkyl berberine analogues intercalated to DNA much stronger than berberine, the chain length of the linker plays an important role for the binding, and they induced ROS mediated apoptosis in HepG2 and MCF-7 cells by p53 modulation.
A new sequential intramolecular cyclization based on the boekelheide rearrangement
Massaro, Assunta,Mordini, Alessandro,Mingardi, Anna,Klein, Jens,Andreotti, Daniele
experimental part, p. 271 - 279 (2011/02/28)
Pyrrolidines and piperidines were synthesized from (aminoalkyl)pyridine N-oxides with a general and quite efficient method developed by using di-tert-butylsilyl bis(trifluoromethanesulfonate) as a new promoter for a Boekelheide-type reaction. The use of a
Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist
Kitbunnadaj, Ruengwit,Zuiderveld, Obbe P.,Christophe, Bernard,Hulscher, Saskia,Menge, Wiro M. P. B.,Gelens, Edith,Snip, Erwin,Bakker, Remko A.,Celanire, Sylvain,Gillard, Michel,Talaga, Patrice,Timmerman, Henk,Leurs, Rob
, p. 2414 - 2417 (2007/10/03)
In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at the human histamine H3 receptor. Particularly, the 4-
Synthesis and Structure-Activity Relationships of Conformationally Constrained Histamine H3 Receptor Agonists
Kitbunnadaj, Ruengwit,Zuiderveld, Obbe P.,De Esch, Iwan J. P.,Vollinga, Roeland C.,Bakker, Remko,Lutz, Martin,Spek, Anthony L.,Cavoy, Emile,Deltent, Marie-France,Menge, Wiro M. P. B.,Timmerman, Henk,Leurs, Rob
, p. 5445 - 5457 (2007/10/03)
Immepip, a conformationally constrained analogue of the histamine congener imbutamine, shows high affinity and functional activity on the human H 3 receptor. Using histamine and its homologues as prototypes, other rigid analogues containing eit
Antagonists of gonadotropin releasing hormone
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, (2008/06/13)
There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists
Lin, Peter,Parikh, Mamta,Lo, Jane-Ling,Yang, Yi Tien,Cheng, Kang,Smith, Roy G,Fisher, Michael H,Wyvratt, Matthew J,Goulet, Mark T
, p. 1077 - 1080 (2007/10/03)
A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3,5-dimethylphenyl)tr
Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus
Ashton, Wallace T.,Sisco, Rosemary M.,Yang, Yi Tien,Lo, Jane-Ling,Yudkovitz, Joel B.,Gibbons, Patrice H.,Mount, George R.,Ren, Rena Ning,Butler, Bridget S.,Cheng, Kang,Goulet, Mark T.
, p. 1727 - 1731 (2007/10/03)
A pyridine side-chain terminus has been incorporated into the indole-5-carboxamide and indole-5-acetamide series of GnRH antagonists. Potent activity was observed in binding and functional assays. Certain branched or cyclic tertiary amides were identified
Antagonists of gonadotropin releasing hormone
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, (2008/06/13)
There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
