Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers.

Richard K Amewu; James Chadwick; Afthab Hussain; Somnath Panda; Rinki Rinki; Omar Janneh; Stephen A Ward; Candel Miguel; Hollie Burrell-Saward; Livia Vivas; +1 more... Paul M O'Neill; (2013) Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers. Bioorganic & medicinal chemistry, 21 (23). pp. 7392-7397. ISSN 0968-0896 DOI: 10.1016/j.bmc.2013.09.047
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The synthesis of a range of mono spiro and dispiro 1,2,4,5-tetraoxane dimers is described. Selected molecules were examined in in vitro assays to determine their antimalarial and anticancer potential. Our studies reveal that several molecules possess potent nanomolar antimalarial and single digit micromolar antiproliferative IC(50)s versus colon (HT29-AK and leukemia (HL60) cell lines.

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