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
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor
Wallace-Povirk, Adrianne,Tong, Nian,Wong-Roushar, Jennifer,O'Connor, Carrie,Zhou, Xilin,Hou, Zhanjun,Bao, Xun,Garcia, Gloria E.,Li, Jing,Kim, Seongho,Dann, Charles E.,Matherly, Larry H.,Gangjee, Aleem
, (2021/03/29)
We discovered 6-substituted thieno[2,3-d]pyrimidine compounds (3–9) with 3–4 bridge carbons and side-chain thiophene or furan rings for dual targeting one-carbon (C1) metabolism in folate receptor- (FR) expressing cancers. Synthesis involved nine steps st
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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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.