74684-38-1Relevant academic research and scientific papers
Phospholane-Phosphite Ligands for Rh Catalyzed Enantioselective Conjugate Addition: Unusually Reactive Catalysts for Challenging Couplings
Clarke, Matthew L.,Cordes, David B.,Fuentes, José A.,Gilbert, Sophie H.,Slawin, Alexandra M. Z.
supporting information, (2020/05/25)
The use of Rh catalysts derived from a phospholane-phosphite ligand were found to be more productive than the classic rhodium/BINAP system in enantioselective conjugate additions. These catalysts enable the use of lower amounts of aryl boronic acid in an
ALPHAvBETA1 INTEGRIN ANTAGONISTS
-
Paragraph 0238, (2020/01/31)
The present disclosure provides pharmaceutical agents, including those of the formula: (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents are also provided. The compounds may be used for the inhibition or antagonism of integrins ανβ1 and/or α5β1. In some embodiments, the compounds provided herein exhibit reduced inhibitory or antagonistic activity of integrins ανβ3, ανβ5, ανβ6, ανβ8, and/or αIIbβ3.
Photosensitive porphyrin dyes for dye-sensitized solar cells
-
Page/Page column 29, (2017/07/14)
A photosensitive porphyrin-based dye is adapted to be used in a photoelectric converting device such as a dye-sensitized solar cell. The photosensitive porphyrin-based dye has a porphyrin center, at least one electron donor unit, at least one electron acc
PHOTOSENSITIVE PORPHYRIN DYES FOR DYE-SENSITIZED SOLAR CELLS
-
, (2016/03/05)
A photosensitive porphyrin-based dye is adapted to be used in a photoelectric converting device such as a dye-sensitized solar cell. The photosensitive porphyrin-based dye has a porphyrin center, at least one electron donor unit, at least one electron acc
New hydroxystilbenoid derivatives endowed with neuroprotective activity and devoid of interference with estrogen and aryl hydrocarbon receptor-mediated transcription
Villalonga-Barber, Carolina,Meligova, Aggeliki K.,Alexi, Xanthippi,Steele, Barry R.,Kouzinos, Constantinos E.,Screttas, Constantinos G.,Katsanou, Efrosini S.,Micha-Screttas, Maria,Alexis, Michael N.
supporting information; experimental part, p. 339 - 351 (2011/02/27)
We have synthesized a series of new (E) stilbenoid derivatives containing hydroxy groups at ring positions identical or similar to those of trans-resveratrol and bearing one or two bulky electron donating groups ortho to 4′-OH and we have evaluated their neuroprotective activity using glutamate-challenged HT22 hippocampal neurons to model oxidative stress-induced neuronal cell death. The most active derivatives, 5-{(E)-2-[3,5-bis(1- ethylpropyl)-4-hydroxyphenyl]ethenyl}-1,3-benzenediol (2), 5-[(E)-2-(3,5-di- tert-butyl-4-hydroxyphenylethenyl)]-1,3-benzenediol (4) and 5-{(1E,3E)-4-[3,5- bis(1-ethylpropyl)-4-hydroxyphenyl]-1,3-butadienyl}-1,3-benzenediol (6), had EC50 values of 30, 45 and 12 nM, respectively, and were ca. 100 to 400-fold more potent than resveratrol. Derivatives 2, 4 and 6 lacked cytotoxic activity against HT22 cells and estrogen receptor agonist or antagonist activity in estrogen response element-dependent gene expression and in estrogen-dependent proliferation of MCF-7 human breast cancer cells. In addition, they were incapable of interfering with aryl hydrocarbon receptor-mediated xenobiotic response element-dependent gene expression. Derivatives 2, 4 and 6 might assist in the development of lead candidates against oxidative stress-driven neurodegenerative diseases that will not increase endocrine cancer risk nor affect drug activation and detoxification mechanisms.
Development of one-pot synthesis of new antiarthritic drug candidate S-2474 with high E-selectivity
Oda, Katsuo,Hida, Takemasa,Sakata, Terao,Nagai, Masahiko,Sugata, Yoshihide,Masui, Toshiaki,Nogusa, Hideo
, p. 442 - 446 (2013/01/03)
A one-pot synthesis of S-2474 was developed to overcome the problems of a large number of steps, low stereoselectivity, low yield, a large amount of waste, and severe reaction conditions. Aldol-type condensation of 3,5-di-terf-butyl-4-hydroxybenzaldehyde and iV-ethyl-γsultam was carried out with LDA and then quenched with water. Dehydration proceeded under basic conditions, providing S-2474 directly as a single isomer on the benzylidene double bond. The reaction mechanism appears to involve a quinone methide intermediate. Environmental assessment of the development of this compound is also discussed in this paper.
Mechanistic and steric issues in the oxidation of phenolic and non-phenolic compounds by laccase or laccase-mediator systems. the case of bifunctional substrates
D'Acunzo, Francesca,Galli, Carlo,Gentili, Patrizia,Sergi, Federica
, p. 583 - 591 (2007/10/03)
Steric and redox issues of phenolic and non-phenolic substrates are investigated for a better insight of the reactivity features of the phenoloxidase laccase. Whenever a substrate is endowed with a redox potential too high for direct monoelectronic oxidation by the enzyme, or else is too much encumbered to access the enzymatic pocket, redox mediators overcome the problem, behaving as an interface between enzyme and substrate. For example, the small-sized mediator ABTS, once oxidised by laccase, fruitfully interacts with bulky substrates, 2,4,6-tri(But)-phenol providing a significant case. Other mediators, for example HBT, resort to a radical oxidation mechanism precluded to laccase, and can react with non-phenolic substrates which are impossible for the enzyme. The advantages provided by the mediators are discussed, and suitable phenolic compounds, as precursors of phenoxyl radical intermediates, emerge as a new proficient class. They could be the true natural mediators of laccase in the oxidative delignification. In fact, phenoxyl radical fragments generated by laccase from lignin, or from phenolic monomer residuals from the building up of lignin polymer or else deriving from lignin by oxidation with other ligninolytic enzymes, could oxidise non-phenolic residues of lignin thereby causing the breakdown of its alkyl network. The novel mechanistic probe 3,5-di(But)-4-OH-benzyl alcohol enables the decoupling of the reactivity channels of a phenolic vs. a benzylic alcohol moiety in the enzymatic oxidation of bifunctional substrates having structural features comparable to portions of lignin. Experimental support is thereby attained for the central role of laccase in biodelignification, in spite of the seemingly lower oxidation power of this enzyme with respect to other and stronger oxidising enzymes excreted by ligninolytic fungi. the Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2006.
Synthesis and characterization of BHT-derived tert-butyl dendrons
Shanahan, Charles S.,McGrath, Dominic V.
, p. 1054 - 1056 (2007/10/03)
(Chemical Equation Presented) A series of 3,5-poly(aryl ether) dendrons was prepared up to the third generation using inexpensive 3,5-di-tert-butyl-4- hydroxytoluene (BHT, 1) as a starting material.
TX-1123: An antitumor 2-hydroxyarylidene-4-cyclopentene-1,3-dione as a protein tyrosine kinase inhibitor having low mitochondrial toxicity
Hori, Hitoshi,Nagasawa, Hideko,Ishibashi, Masaki,Uto, Yoshihiro,Hirata, Akihiko,Saijo, Kouichi,Ohkura, Kazuto,Kirk, Kenneth L,Uehara, Yoshimasa
, p. 3257 - 3265 (2007/10/03)
A series of 2-hydroxyarylidene-4-cyclopentene-1,3-diones were designed, synthesized, and evaluated with respect to protein tyrosine kinase (PTK) inhibition, mitochondrial toxicity, and antitumor activity. Our results show that the cyclopentenedione-derived TX-1123 is a more potent antitumor tyrphostin and also shows lower mitochondrial toxicity than the malononitrile-derived AG17, a potent antitumor tyrphostin. The O-methylation product of TX-1123 (TX-1925) retained its tyrphostin-like properties, including mitochondrial toxicity and antitumor activities. However, the methylation product of AG17 (TX-1927) retained its tyrphostin-like antitumor activities, but lost its mitochondrial toxicity. Our comprehensive evaluation of these agents with respect to protein tyrosine inase inhibition, mitochondrial inhibition, antitumor activity, and hepatotoxicity demonstrates that PTK inhibitors TX-1123 and TX-1925 are more promising candidates for antitumor agents than tyrphostin AG17. Copyright
Steric Effects of Meta Substituents in Substituted Tetraphenylporphyrin Complexes of Ruthenium, Indium, Titanium, and Gallium
Shroyer, A. Laurie W.,Lorberau, Charles,Eaton, Sandra S.,Eaton, Gareth R.
, p. 4296 - 4302 (2007/10/02)
The ruthenium carbonyl 4-tert-butylpyridine, indium, chloride, titanyl, and gallium chloride complexes of tetrakis(3,4,5-trimethoxyphenyl)porphyrin and tetrakis(3,5-dimethoxyphenyl)porphyrin and the ruthenium carbonyl 4-tert-butylpyridine, titanyl, and ga
