169339-41-7Relevant articles and documents
Cyclin-dependent kinase inhibitors and application thereof
-
Paragraph 0241; 0243; 0244; 0245, (2018/07/30)
The invention relates to compounds used as cyclin-dependent kinase inhibitors and application thereof, belonging to the field of medical chemistry. Specifically, the invention provides the compound asshown in a formula I which is described in the specification, or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, preparation methods thereof, pharmaceutical compositions containing the compounds, and application of the compounds or the compositions to treatment of cancer, tissue hyperplasia diseases or inflammatory diseases. The compounds of the invention havegood inhibitory activity to CDK7 and are highly expected to be developed into a therapeutic agent for cancer, tissue hyperplasia diseases and inflammatory diseases.
PYRIMIDINE DERIVATIVE
-
Page/Page column 172, (2010/11/25)
A compound represented by the general formula (1) which has an inhibitory effect on PDE4 activity and produces little adverse side effects: wherein Ar1 represents a furyl, thienyl, triazolyl, thiazolyl, oxazolyl or benzothiazolyl group; Ar2 represents -E-AR21-G-Q (where Ar21 represents a benzene or naphthalene ring; E represents a single bond or an alkylene group; G represents a single bond, an alkylene group or an alkenylene group; and Q represents a carboxyl group, -CON(R41)(R42) or -COOR43), -E-Ar21-G2-G-Q (where E, Ar21, G and Q are as defined above; and G2 represents -O-, -S-, -SO-, -SO2- or -NRG21-) or a monocyclic aromatic heterocyclic ring other than a pyrazolyl group; R1 and R2 are the same as or different from each other and independently represent a hydrogen atom, an alkyl group which may be substituted or the like; and R3 represents a hydrogen atom or an alkyl group which may be substituted.
A Convergent Synthesis of 14-Membered F-O-G Ring Analogs of the Teicoplanin Binding Pocket via Intramolecular SNAr Reaction
Zhu, Jieping,Beugelmans, Rene,Bourdet, Sebastien,Chastanet, Jacqueline,Roussi, George
, p. 6389 - 6396 (2007/10/03)
An intramolecular SNAr reaction for efficient macrocyclization via biaryl ether formation was developed for syntheses of the 14-membered macrocycles 2 and 3 related to F-O-G ring of teicoplanin 1.Chloride as well as fluoride could be used as the leaving group in this reaction.However, the latter was prefered since it required milder conditions.Both ortho and para nitro, fluoro disubstituted aromatic rings were suitable for the macrocyclization reaction with tethered aryl oxides.The nonproteinogenic α-amino acid 23, required for the synthesis of 3, was prepared via an asymmetric Strecker synthesis using (R)-phenylglycinol as a chiral auxiliary.The overall synthetic strategy was convergent, and the cyclization could be performed in the presence of the highly sensitive arylglycine unit without racemization.