Synthesis and biological evaluation of novel naphthoquinone fused cyclic aminoalkylphosphonates and aminoalkylphosphonic monoester |
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Authors: | B. Wang Z. W. Miao J. Wang R. Y. Chen X. D. Zhang |
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Affiliation: | College of Pharmaceutical Sciences, Nankai University, Tianjin, China. binwang@mail.nankai.edu.cn |
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Abstract: | A series of novel naphthoquinone fused cyclic alpha-aminophosphonates, 2-alkoxy-3,4-dihydro-2H-naphtho[2,3-e][1,4,2]oxazaphosphinane-5,10-dione 2-oxide 3-17 and naphthoquinone fused cyclic alpha-aminophosphonic monoester 18 were synthesized for the first time. These cyclic alpha-aminophosphonates were evaluated for antitumor activity on four human tumor cell lines, and three of them showed significant cytotoxicity (IC(50): 0.019-5.15 microM) comparable to that of the reference drug doxorubicin. Furthermore, inhibition assays for topoisomerase II-mediated relaxation of supercoiled DNA indicated that the naphthoquinone fused cyclic aminophosphonates were catalytic inhibitors of topoisomerase II. |
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