98437-13-9Relevant academic research and scientific papers
Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors
Ibrahim, Diaa A.,Ismail, Nasser S.M.
experimental part, p. 5825 - 5832 (2011/12/22)
The design and synthesis of a small library of 4-aminopyrido[2,3-d] pyrimidine derivatives is reported. The potential activity of these compounds as CDK2/Cyclin A, CDK4/Cyclin D, EGFR and anti-tumor was evaluated by cytotoxicity studies in A431a, SNU638b, HCT116 and inhibition of CDK2-Cyclin A, CDK4/Cyclin D and EGFR enzyme activity in vitro. The anti-proliferative and CDK2-Cyclin A inhibitory activity of compounds 4c and 11a was significantly more active than roscovotine with IC50 0.3 and 0.09 μM respectively. Molecular modeling study, including fitting to a 3D-pharmacophore model, docking into cyclin dependant kinase2 (CDK2) active site and binding energy calculations were carried out and these studies suggested the same binding orientation inside the CDK2 binding pocket for these analogs compared to ATP.
Synthesis of highly substituted pyridines via a one-pot, three-component cascade reaction of malononitrile with aldehydes and S-alkylisothiouronium salts in water
Wang, Zhong-Qing,Ge, Ze-Mei,Cheng, Tie-Ming,Li, Run-Tao
experimental part, p. 2020 - 2022 (2009/12/29)
A novel methodology for the synthesis of 2-amino-4-aryl(alkyl)-6-sulfanyl pyridine-3,5-dicarbonitriles via a one-pot, three-component reaction of structurally diversified aldehydes with various S-alkylisothiouronium salts and malononitrile in water has be
CYCLIZATION OF NITRILES. XXV. SYNTHESIS AND REACTIONS OF CHALCOGEN-CONTAINING 6-AMINO-3,5-DICYANOPYRIDINES
Sharanin, Yu. A.,Shestopalov, A. M.,Litvinin, V. P.,Klokol, G. V.,Mortikov, V. Yu.,Demerkov, A. S.
, p. 771 - 776 (2007/10/02)
Methods were developed for the synthesis of 6-amino-3,5-dicyano-2(1H)-pyridinethiones and the corresponding selenones by the reaction of β-alkoxy- or β-aminomethylenemalonitriles with cyanothio(seleno)acetamides.The salts of pyridine-2-thiolates are alkylated selectively by halogenoalkanes with the formation of 2-alkylthiopyridines, which were used in the synthesis of 3-aminothienopyridines and quaternized thiazolopyridines.
