2013 |
Castro-Castillo, V; Suarez-Rozas, C; Castro-Loiza, N; Theoduloz, C; Cassels, B K Annulation of Substituted Anthracene-9,10-Diones Yields Promising Selectively Antiproliferative Compounds Artículo de revista European Journal of Medicinal Chemistry, 62 , pp. 688-692, 2013, ISSN: 0223-5234. Resumen | Enlaces | BibTeX | Etiquetas: activity, anthracene-9, anticancer antiproliferative binding crystal-structure, cytotoxic derivatives, oxoisoaporphines, synthetic @article{RN124, title = {Annulation of Substituted Anthracene-9,10-Diones Yields Promising Selectively Antiproliferative Compounds}, author = { V. Castro-Castillo and C. Suarez-Rozas and N. Castro-Loiza and C. Theoduloz and B.K. Cassels}, url = {/brokenurl#<Go to ISI>://WOS:000318577500069}, doi = {10.1016/j.ejmech.2013.01.049}, issn = {0223-5234}, year = {2013}, date = {2013-01-01}, journal = {European Journal of Medicinal Chemistry}, volume = {62}, pages = {688-692}, publisher = {2013 Elsevier Masson SAS.}, abstract = {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.}, keywords = {activity, anthracene-9, anticancer antiproliferative binding crystal-structure, cytotoxic derivatives, oxoisoaporphines, synthetic}, pubstate = {published}, tppubtype = {article} } 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. |
2013 |
Annulation of Substituted Anthracene-9,10-Diones Yields Promising Selectively Antiproliferative Compounds Artículo de revista European Journal of Medicinal Chemistry, 62 , pp. 688-692, 2013, ISSN: 0223-5234. |