1459-50-3Relevant academic research and scientific papers
Rice (Oryza sativa) tir1 and 5′adamantyl-iaa significantly improve the auxin-inducible degron system in schizosaccharomyces pombe
Watson, Adam T.,Hassell-Hart, Storm,Spencer, John,Carr, Antony M.
, (2021)
The auxin-inducible degron (AID) system is a powerful tool to induce targeted degradation of proteins in eukaryotic model organisms. The efficiency of the existing Schizosaccharomyces pombe AID system is limited due to the fusion of the F-box protein TIR1
Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid
Mélin, Léa,Abdullayev, Shuay,Fnaiche, Ahmed,Vu, Victoria,González Suárez, Narjara,Zeng, Hong,Szewczyk, Magdalena M.,Li, Fengling,Senisterra, Guillermo,Allali-Hassani, Abdellah,Chau, Irene,Dong, Aiping,Woo, Simon,Annabi, Borhane,Halabelian, Levon,LaPlante, Steven R.,Vedadi, Masoud,Barsyte-Lovejoy, Dalia,Santhakumar, Vijayaratnam,Gagnon, Alexandre
, p. 2982 - 3002 (2021/08/03)
The YAP-TEAD transcriptional complex is responsible for the expression of genes that regulate cancer cell growth and proliferation. Dysregulation of the Hippo pathway due to overexpression of TEAD has been reported in a wide range of cancers. Inhibition of TEAD represses the expression of associated genes, demonstrating the value of this transcription factor for the development of novel anti-cancer therapies. We report herein the design, synthesis and biological evaluation of LM98, a flufenamic acid analogue. LM98 shows strong affinity to TEAD, inhibits its autopalmitoylation and reduces the YAP-TEAD transcriptional activity. Binding of LM98 to TEAD was supported by 19F-NMR studies while co-crystallization experiments confirmed that LM98 is anchored within the palmitic acid pocket of TEAD. LM98 reduces the expression of CTGF and Cyr61, inhibits MDA-MB-231 breast cancer cell migration and arrests cell cycling in the S phase during cell division.
PLANT GROWTH REGULATOR
-
Paragraph 0295-0296, (2021/08/06)
Providing an auxin derivative that can exert its intended effect more efficiently, while reducing any unintended effects. A compound represented by the General Formula (1) having a specific substituent at the 5- and/or 6-position of the auxin indole ring.
Nitrogen-containing compound, electronic element, and electronic device
-
Paragraph 0187; 0199-0201, (2021/03/24)
The invention relates to a nitrogen-containing compound, an electronic element comprising the nitrogen-containing compound, and an electronic device comprising the electronic element. According to thenitrogen-containing compound, an adamantyl group and a bis (triarylamine) structure are combined to form a core structure, the whole molecule forms a large conjugated system, meanwhile, the molecularrigidity is improved, and the thermal stability is remarkably improved. When the nitrogen-containing compound is applied to the electronic element, the luminous efficiency or the power generation efficiency of the electronic element can be improved, and the service life can be prolonged.
NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS
-
Page/Page column 106, (2020/10/09)
The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.
Adamantylation of N-aryl and N-arylalkyl acetamides in trifluoroacetic acid
Kireeva, A. V.,Nakhod, M. A.,Novakov, I. A.,Orlinson, B. S.,Pichugin, A. M.,Porkhun, V. I.,Potaenkova, E. A.,Savelyev, E. N.,Vostrikova, O. V.,Zavyalov, D. V.
, p. 1096 - 1101 (2020/07/25)
Alkylation of N-aryl and N-arylalkyl acetamides with hydroxy adamantane derivatives in trifluoroacetic acid was studied. The differentiating effect of trifluoroacetic acid on the regio-selectivity of adamantylation of o-alkyl-substituted acetanilides was established, leading to energetically more stable products of para-substitution with respect to the alkyl group (the content of para-alkyl isomers is 93–94percent). This enabled the synthesis of adamantylaminoarenes in 83–99percent yields and with 95–99percent purity.
Synthesis and reactions of some 5(6)-(1-adamantyl)benzimidazoles
Zurabishvili,Lomidze,Samsoniya,Wesquet,Kazmaier
experimental part, p. 941 - 949 (2009/05/26)
4-(1-Adamantyl)-1,2-diaminobenzene, previously unreported in the literature, has been prepared and a novel series of 5(6)-(1-adamantyl) benzimidazole derivatives synthesized. Nitration, hydrogenation, and side chain reactions have been carried out.
TRIFLUOROACETIC ANHYDRIDE AS A MEDIUM FOR ORGANIC REACTIONS. FUNCTIONAL SUBSTITUTION OF ADAMANTANE AND ITS DERIVATIVES
Kovalev, V. V.,Fedorova, O. A.,Shokova, E. A.
, p. 1672 - 1675 (2007/10/02)
The role of trifluoroacetic anhydride during the oxidation of adamantane and its derivatives with sulfuric acid was studied. 1-Adamantanol, 1-(4-methyl-3-nitrophenyl)-3-adamantanol.The latter was used without isolation from the reaction mixture for the production of 1-adamantanecarboxylic acid, N-(1-adamantyl)acetamide, 1-(1-adamantyl)butan-1-ol, 1-(4-methylphenyl)adamantane, 4-(1-adamantyl)phenoxyacetic acid, 4-(1-adamantyl)acetanilide, and 4-(1-adamantyl)bromobenzene.
KINETICS OF THE ACYLATION OF MONOSUBSTITUTED AROMATIC AMINES BY ACID CHLORIDES
Khardin, A. P.,Novakov, I. A.,Radchenko, S. S.,Brel', N. A.,Chegolya, A. S.,et al.
, p. 1492 - 1495 (2007/10/02)
The kinetics of the acylation of p-toluidine and 1-(4-aminophenyl)adamantane by acid chlorides were investigated.It was established that adamantanecarbonyl chlorides have lower reactivity than cyclohexanecarbonyl chlorides and aliphatic acid chlorides.
