62224-19-5Relevant articles and documents
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors
Zhan, Wenhu,Che, Jinxin,Xu, Lei,Wu, Yizhe,Hu, Xiaobei,Zhou, Yubo,Cheng, Gang,Hu, Yongzhou,Dong, Xiaowu,Li, Jia
, p. 72 - 85 (2019)
A series of pyrazole-thiophene derivatives exhibiting good Akt inhibitory activities were obtained on the basis of conformational restriction strategy, leading to the discovery of compound 1d and 1o which showed excellent in vitro antitumor effect against a variety of hematologic cancer cells and their potential of inducing apoptosis, blocking the cell cycles at S phase and significantly inhibiting the phosphorylation of downstream biomarkers of Akt kinase of cancer cells. Amongst, compound 1o also exhibited good PK profiles and inhibited about 40% tumor growth in MM1S xenograft model. Compound 1o might be a potential candidate for further development.
Redox states of well-defined π-conjugated oligothiophenes functionalized with poly(benzyl ether) dendrons
Apperloo, Joke J.,Janssen, Rene A.J.,Malenfant, Patrick R.L.,Groenendaal, Lambertus,Frechet, Jean M.J.
, p. 7042 - 7051 (2000)
The redox states of a series of well-defined hybrid dendrimers based on oligothiophene cores and poly(benzyl ether) dendrons have been studied using cyclic voltammetry and variable-temperature UV/visible/ near-IR spectroscopy. The oxidation potentials and
Ag(I)-Catalyzed C-H Carboxylation of Thiophene Derivatives
Lee, Mijung,Hwang, Young Kyu,Kwak, Jaesung
supporting information, p. 3136 - 3144 (2021/09/30)
CO2utilization is an attractive aspect as it allows the direct conversion of CO2into valuable chemicals. In this regard, direct incorporation of CO2into the C-H bond of heteroaromatic compounds is important due to the ubiquitous structural motifs of the heteroaromatic carboxylic acids. Herein, we report the Ag-catalyzed C-H carboxylation of thiophene derivatives. This new catalytic system involving a phosphine ligand and lithiumtert-butoxide enables the direct carboxylation of thiophenes under mild reaction conditions. Experimental studies revealed that the use oftert-butyl alkoxide is critical for the exergonic formation of an arylsilver intermediate, and the results were further supported by density functional theory calculations.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
-
Paragraph 00230; 00478, (2020/07/05)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.