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Author: search.filters.author.Gleeson, M. PaulSubject: search.filters.subject.A549

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    Item type:Publication,
    Synthesis and evaluation of the NSCLC anti-cancer activity and physical properties of 4-aryl-N-phenylpyrimidin-2-amines
    (2017-01-01)
    Toviwek, Borvornwat
    ;
    Suphakun, Praphasri
    ;
    Choowongkomon, Kiattawee
    ;
    Hannongbua, Supa
    ;
    Gleeson, M. Paul
    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 (logD<inf>7.4</inf> 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 logD<inf>7.4</inf> (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.