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  • Title: Methylenebisphosphonates with dienone pharmacophore: synthesis, structure, antitumor and fluorescent properties.
    Author: Makarov MV, Leonova ES, Rybalkina EY, Khrustalev VN, Shepel NE, Röschenthaler GV, Timofeeva TV, Odinets IL.
    Journal: Arch Pharm (Weinheim); 2012 May; 345(5):349-59. PubMed ID: 22213431.
    Abstract:
    The synthesis and the antitumor activity and fluorescent properties screening of novel bisphosphonate conjugates with cytotoxic 3,5-bis((hetero)arylidene)-4-piperidone residues were performed. The facile and rapid synthetic route was based on the aza-Michael addition of NH-3,5-bis((hetero)arylidene)-4-piperidones to tetraethyl ethylidenebisphosphonate. The synthesized compounds displayed high inhibitory properties towards Caov3, A549, PC3, and KB 3-1 human carcinoma cell lines. Among those, compounds bearing 4-cyano-phenyl and 3-pyridinyl substituents were revealed as the most active drug candidates with IC(50) values in the range of 0.5-2.5 µM. Methylenebisphosphonate with 4-Me(2) N-C(6) H(4) groups in the piperidone framework possessing fluorescence properties may be of interest for visualization of BPs skeletal distribution and cellular uptake in bones and other tissues.
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