Annulation of substituted anthracene-9,10-diones yields promising selectively antiproliferative compounds
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Anthraquinone derivatives are well-known antiproliferative compounds, and some are currently used in cancer chemotherapy. Some families of annulated anthraquinone analogs have also been examined for antiproliferative activity, but in this regard almost nothing is known of 1-azabenzanthrones (7H-dibenzo [de,h]quinolin-7-ones). A series of 1-azabenzanthrone derivatives, their 2,3-dihydro analogs, and congruently substituted 9,10-anthracenediones were tested against normal human fibroblasts and four human cancer cell lines. Most of the heterocyclic compounds proved to be weakly to moderately antiproliferative with 1050 values extending down to 0.86 mu M, and exhibited up to 30-fold selectivity between cancer and normal cells. Both 1-azabenzanthrones and 1-aza-2,3-dihydrobenzanthrones were more potent than their anthraquinone counterparts, and almost without exception, the 2,3-dihydro compounds were more potent than the fully aromatic 1-azabenzanthrones
Artículo de publicación ISI
MeceSup (UMCE-0204) fellowship. This work was supported by CONICYT grant AT-23070040 and ICM grant P05-001-F.
DOI: doi: 10.1016/j.ejmech.2013.01.049
Quote ItemEuropean Journal of Medicinal Chemistry 62 (2013) 688-692