126940-10-1Relevant academic research and scientific papers
Myxochelin-Inspired 5-Lipoxygenase Inhibitors: Synthesis and Biological Evaluation
Schieferdecker, Sebastian,K?nig, Stefanie,Pace, Simona,Werz, Oliver,Nett, Markus
, p. 23 - 27 (2017)
A total of 48 analogues of the natural product myxochelin A were prepared and evaluated for their inhibitory effects on human 5-lipoxygenase in both cell-free and cell-based assays. Structure–activity relationship analysis revealed that the secondary alcohol function and only chiral center of myxochelin A is not required for biological activity. By expanding the diaminoalkane linker of the two aromatic residues it was possible to generate a myxochelin derivative with superior activity against 5-lipoxygenase in intact cells.
Harnessing Enzymatic Promiscuity in Myxochelin Biosynthesis for the Production of 5-Lipoxygenase Inhibitors
Korp, Juliane,K?nig, Stefanie,Schieferdecker, Sebastian,Dahse, Hans-Martin,K?nig, Gabriele M.,Werz, Oliver,Nett, Markus
, p. 2445 - 2450 (2015)
The siderophore myxochelin A is a potent inhibitor of human 5-lipoxygenase (5-LO). To clarify whether the iron-chelating properties of myxochelin A are responsible for this activity, several analogues of this compound were generated in the native producer Pyxidicoccus fallax by precursor-directed biosynthesis. Testing in a cell-free assay unveiled three derivatives with bioactivity comparable with that of myxochelin A. Furthermore, it became evident that inhibition of 5-LO by myxochelins does not correlate with their iron affinities. A series of new myxochelin analogues was generated by precursor-directed biosynthesis. Some derivatives possess only weak iron-chelating properties, but are still potent inhibitors of human 5-lipoxygenase, an enzyme featuring a non-heme iron atom in its catalytically active site.
TRICYCLIC INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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Paragraph 00238, (2019/07/13)
The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
INHIBITORS OF THE BCL6 BTB DOMAIN PROTEIN-PROTEIN INTERACTION AND USES THEREOF
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Paragraph 00288, (2019/08/29)
The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.
SEROTONERGIC BENZOTHIOPHENES
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Page 19, (2010/02/08)
The present invention provides serotonergic benzothiophenes of Formula (I), where A, R, R, R, R, and R are as described in the specification.
Fluorophenols and (trifluoromethyl)phenols as substrates of site-selective metalation reactions: To protect or not to protect
Marzi, Elena,Mongin, Florence,Spitaleri, Andrea,Schlosser, Manfred
, p. 2911 - 2915 (2007/10/03)
O-Methoxymethyl (MOM) protected fluorophenols can be cleanly metalated and subsequently be submitted to site-selective electrophilic substitution. The 2- and 4-isomers exhibit ambivalent reactivity: deprotonation occurs at the position adjacent to the oxygen when butyllithium is employed whereas the position adjacent to the fluorine is attacked by the superbasic mixture of butyllithium and potassium tert-butoxide (LIC-KOR). The MOM-protected (trifluoromethyl)-phenols react exclusively at oxygen-neighboring positions. The meta isomer provides another example of optional site selectivity, undergoing hydrogen/metal exchange at the 2-position with the LIC-KOR reagent and at the 6-position with sec-butyllithium. Unprotected (trifluoromethyl)phenols can also be ortho-metalated after O-deprotonation, although the products are formed in only moderate yields.
Synthesis of constrained arylpiperidines using intramolecular Heck or radical reactions
Morice, Christophe,Domostoj, Mathias,Briner, Karin,Mann, André,Suffert, Jean,Wermuth, Camille-Georges
, p. 6499 - 6502 (2007/10/03)
Two intramolecular routes were experimented to reach the hexahydrobenzofuro[2,3-c]pyridine platform: a Heck and a radical reaction. The radical route was applicable to all substrates, whereas the Heck route was of limited use. The key adducts were obtained via a Mitsunobu condensation between halogenated phenols and an allylic alcohol, the 3-hydroxy-tetrahydropyridine.
A Novel Synthesis of 3-Amino-1,2-benzisoxazoles - an Entry into the Isoxazolobenzoxazepine Ring System
Shutske, Gregory M.,Kapples, Kevin J.
, p. 1293 - 1298 (2007/10/02)
A novel synthesis of 3-amino-1,2-benzisoxazole (3) from 2-benzonitrile (2) is described.This methodology was used to synthesize 3-amino-4-hydroxy-1,2-benzisoxazole (10), which served as an intermediate for a number of isoxazolo3
