75634-04-7Relevant articles and documents
Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines
Toviwek, Borvornwat,Suphakun, Praphasri,Choowongkomon, Kiattawee,Hannongbua, Supa,Gleeson, M. Paul
supporting information, p. 4749 - 4754 (2017/09/29)
Reported herein are efforts to profile 4-aryl-N-phenylpyrimidin-2-amines in terms of their anti-cancer activity towards non small-cell lung carcinoma (NSCLC) cells. We have synthesized new 4-aryl-N-phenylpyrimidin-2-amines and assessed them in terms of their cytotoxicity (A549, NCI-H187, MCF7, Vero & KB) and physicochemical properties (logD7.4 and solubility). 13f and 13c demonstrated potent anti-cancer activity in A549 cells (0.2 μM), compared to 0.4 μM for the NSCLC drug Doxorubicin. 13f also displayed low experimental logD7.4 (2.9) and the best solubility (~40 μM). Compounds 13b and 13d showed the best balance of A549 anti-cancer activity and selectivity. 13g showed good activity and selectivity comparable with the anti-cancer drug Doxorubicin.
Convenient preparation of 4-aryl-2-(heteroarylamino)pyrimidines and 4-anilino-2-(heteroarylamino)pyrimidines
Bliss, Brian I.,Ahmed, Feryan,Iyer, Subashree,Lin, Weimin,Walker, Joel,Zhao, He
supporting information; experimental part, p. 3259 - 3262 (2010/07/10)
4-Aryl-2-anilinopyrimidines and 2,4-dianilinopyrimidines are privileged structures found in many drug-like molecules and biologically active compounds. A method for the quick assembly of novel 4-aryl- and 4-anilino-2-(heteroarylamino)pyrimidines via Buchwald-Hartwig N-arylations at elevated temperatures under sealed tube conditions is reported. This method's convenience and practicality is demonstrated through the preparation of several novel non-nucleoside reverse transcriptase inhibitor (NNRTI) analogues.
Synthesis of 4-substituted 2-(4-methylpiperazino)pyrimidines and quinazoline analogs as serotonin 5-HT2A receptor ligands
Saczewski, Jaroslaw,Paluchowska, Aldona,Klenc, Jeffrey,Raux, Elizabeth,Barnes, Samuel,Sullivan, Shannon,Duszynska, Beata,Bojarski, Andrzej J.,Strekowskia, Lucjan
experimental part, p. 1259 - 1265 (2010/03/23)
(Chemical Equation Presented) The addition reaction of lithium reagents to the 4 position of 2-chloropyrimidine or 2-chloroquinazoline followed by oxidation of the resultant dihydro intermediate product is a powerful tool for the synthesis of 4-substitute