- Partial reduction of pyridinium salts as a versatile route to dihydropyridones
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(Chemical Equation Presented) The addition of two electrons to a pyridinium salt turns it into a nucleophile. The intermediate generated by the reduction of such salts can be reacted successfully with a range of different electrophiles (acids, alkyl halid
- Donohoe, Timothy J.,Johnson, Dale J.,Mace, Laura H.,Bamford, Mark J.,Ichihara, Osamu
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Read Online
- BIARYL DERIVATIVE, PREPARATION METHOD THEREOF AND PHARMACEUTICAL APPLICATION THEREOF
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Disclosed are a biaryl derivative having a structure represented by Formula (I) and inhibitory activity against PD-1/PD-L1 interaction, a preparation method thereof, and a pharmaceutical application thereof. The series of compounds of the present inventio
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Paragraph 0099; 0116; 0117
(2020/12/22)
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- Design of coordination interaction of Zn(II) complex with oligo-aspartate peptide to afford a high-affinity tag-probe pair
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A complementary recognition pair consisting of a genetically encodable peptide tag and a small molecular probe isa powerful tool to specifically label and manipulate a protein ofinterest under biological conditions. In this study, we report the redesign of a tag-probe pair comprising an oligo-aspartate peptide tag (such as DDDD) and a binuclear zinc complex. Isothermal-titration calorimetry screening of binding between the series of peptides and zinc complexes revealed that the binding affinity was largely influenced by subtle changes of the ligand structure of the probe. However, the binding was tolerant to differences of the tag peptide sequence. Of those tested, a pair containing a peptide tag (DDAADD) and a binuclear zinc complex possessing 4-chloropyridines (3-2Zn(II)) showed the strongest binding affinity (Ka = 3.88 × 105 M-1), which was about 10-fold larger than the conventional pair of D4-peptide tag (DDDD) and 1-2Zn(II) containing nonsubstituted pyridines (Ka = 3.73 × 104 M-1). The strong binding of this new complementary recognition pair enabled the rapid covalent labeling of a tag-fused maltose binding protein with a fluorescent zinc complex, demonstrating its potential utility in protein analysis.
- Fuchida, Hirokazu,Tabata, Shigekazu,Shindo, Naoya,Takashima, Ippei,Leng, Qiao,Hatsuyama, Yuji,Hamachi, Itaru,Ojida, Akio
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supporting information
p. 784 - 791
(2015/06/25)
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- COMPOUNDS OF ESTROGEN-RELATED RECEPTOR MODULATORS AND THE USES THEREOF
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The compounds according to formula (I), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modula
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- Scaffold-hopping strategy: Synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents
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Utilizing scaffold-hopping drug-design strategy, we sought to identify a backup drug candidate for BPR0L075 (1), an indole-based anticancer agent. For this purpose, 5,6-fused bicyclic heteroaromatic scaffolds were designed and synthesized through shufflin
- Tung, Yen-Shih,Coumar, Mohane Selvaraj,Wu, Yu-Shan,Shiao, Hui-Yi,Chang, Jang-Yang,Liou, Jing-Ping,Shukla, Paritosh,Chang, Chun-Wei,Chang, Chi-Yen,Kuo, Ching-Chuan,Yeh, Teng-Kuang,Lin, Chin-Yu,Wu, Jian-Sung,Wu, Su-Ying,Liao, Chun-Chen,Hsieh, Hsing-Pang
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supporting information; scheme or table
p. 3076 - 3080
(2011/06/25)
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- Synthesis of cylindricine C and a formal synthesis of cylindricine A
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This paper reports the synthesis of the alkaloid natural product (±)-cylindricine C, in addition to a formal synthesis of (±)-cylindricine A. The key step in our sequence is the (ipso) regioselective addition of an alkyl Grignard reagent to a C-2 substitu
- Donohoe, Timothy J.,Brian, Ptoton M.,Hargaden, Gráinne C.,O'Riordan, Timothy J.C.
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experimental part
p. 6411 - 6420
(2010/10/18)
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- THIAZOLE AND OXAZOLE KINASE INHIBITORS
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The present invention provides thiazole and oxazole compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
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Page/Page column 185
(2009/04/25)
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- Regioselective nucleophilic addition to pyridinium salts: A new route to substituted dihydropyridones
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"Chemical Equation Presented" The regioselective addition of nucleophiles to pyridinium salts generates an intermediate enol-ether, which can be hydrolyzed in situ to provide a range of dihydropyridones. Certain Grignards have shown inherent differences i
- Donohoe, Timothy J.,Connolly, Matthew J.,Walton, Lesley
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supporting information; experimental part
p. 5562 - 5565
(2010/02/28)
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- Quinazoline compounds and pharmaceutical compositions containing them
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The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, NH or NR8 where R8 is hydrogen or C1-6alkyl; Ra is a 3-quinoline group or a group of sub-formula (i) where R5, R6 and R7 are various specific organic groups, in the preparation of a medicament for use in the inhibtion of aurora 2 kinase. Novel compounds of formula (I) and pharmaceutical compositions useful in the treatment of cancer are also described and claimed.
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Page/Page column 45
(2008/06/13)
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- The ammonia-free partial reduction of substituted pyridinium salts
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This paper reports a study into the partial reduction of N-alkylpyridinium salts together with subsequent elaboration of the intermediates thus produced. Activation of a pyridinium salt by placing an ester group at C-2, allows the addition of two electron
- Donohoe, Timothy J.,Johnson, Dale J.,MacE, Laura H.,Thomas, Rhian E.,Chiu, Jessica Y. K.,Rodrigues, Jason S.,Compton, Richard G.,Banks, Craig E.,Tomcik, Peter,Bamford, Mark J.,Ichihara, Osamu
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p. 1071 - 1084
(2007/10/03)
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- Imidazo-pyridine derivatives as ligands for gaba receptors
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A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
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- Aniline derivatives
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The invention concerns aniline derivatives of formula I STR1 wherein m is 1, 2 or 3, n is 0, 1, 2 or 3, Q is phenyl or naphthyl or a 5- or 6-membered heteroaryl moiety containing 1, 2 or 3 heteroatoms selected from oxygen, nitrogen and sulfur, and X, R1 and R2 are defined in the claims; or pharmaceutical compositions containing them, and the methods of using the compounds as tyrosine kinase inhibitors and for the treatment of proliferative diseases such as cancer.
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- A Convenient Synthesis of 1-Methyl-4-oxopipecolic Acid Methyl Ester
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An efficient and convenient synthesis of the title compound 1 is described.The approach to the synthesis is based on hydride reduction of the 4-methoxypyridinium salt 5, followed by acid hydrolysis of the resulting vinyl ether intermediate 6.
- Essawi, M. Y.,Portoghese, P. S.
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p. 477 - 478
(2007/10/02)
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