Browsing by Author "Sinou, V."

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    Synthesis, Characterization, and in vitro Antimalarial and Antitumor Activity of New Ruthenium(II) Complexes of Chloroquine
    (Journal of Inorganic Chemistry, 2009) Rajapakse, C.S.K.; Martínez, A.; Naoulou, B.; Jarzecki, A.A.; Suárez, L.; Deregnaucourt, C.; Sinou, V.; Schrével, J.; Musi, E.; Ambrosini, G.; Schwartz, G.K.; Sánchez-Delgado, R.A.
    The new RuII chloroquine complexes [Ru(?6-arene)(CQ)Cl2] (CQ = chloroquine; arene = p-cymene 1, benzene 2), [Ru(?6-p-cymene)(CQ)(H2O)2][BF4]2 (3), [Ru(?6-p-cymene)(CQ)(en)][PF6]2 (en = ethylenediamine) (4), and [Ru(?6-p-cymene)(?6-CQDP)][BF4]2 (5, CQDP = chloroquine diphosphate) have been synthesized and characterized by use of a combination of NMR and FTIR spectroscopy with DFT calculations. Each complex is formed as a single coordination isomer: In 1?4, chloroquine binds to ruthenium in the ?1-N mode through the quinoline nitrogen atom, whereas in 5 an unprecedented ?6 bonding through the carbocyclic ring is observed. 1, 2, 3, and 5 are active against CQ-resistant (Dd2, K1, and W2) and CQ-sensitive (FcB1, PFB, F32, and 3D7) malaria parasites (Plasmodium falciparum); importantly, the potency of these complexes against resistant parasites is consistently higher than that of the standard drug chloroquine diphosphate. 1 and 5 also inhibit the growth of colon cancer cells, independently of the p53 status and of liposarcoma tumor cell lines with the latter showing increased sensitivity, especially to 1 (IC50 8 ?M); this is significant because this type of tumor does not respond to currently employed chemotherapies