Multidimensional optimization of promising antitumor xanthone derivatives

…, RT Lima, MH Vasconcelos, M Pedro, J Barbosa…

Index: Azevedo, Carlos M.G.; Afonso, Carlos M.M.; Sousa, Diana; Lima, Raquel T.; Helena Vasconcelos; Pedro, Madalena; Barbosa, Joao; Correa, Arlene G.; Reis, Salette; Pinto, Madalena M.M. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 11 p. 2941 - 2959

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Citation Number: 9

Abstract

A promising antitumor xanthone derivative was optimized following a multidimensional approach that involved the synthesis of 17 analogues, the study of their lipophilicity and solubility, and the evaluation of their growth inhibitory activity on four human tumor cell lines. A new synthetic route for the hit xanthone derivative was also developed and applied for the synthesis of its analogues. Among the used cell lines, the HL-60 showed to be in general ...