Abstract:
:A new series of anthracene-9, 10-dione derivatives have been synthesized to increase cytotoxic activity against human papillomavirus (HPV) positive cancer cell line, CaSki. The highest cytotoxicity was achieved by 4-(benzylamino)-9,10-dioxo-4a,9,9a,10-tetrahydroanthracen-1-yl 4-ethylbenzenesulfonate (5) with the inhibitory concentration 50 (IC50) of 0.3 μM which is 20 times lower than that of cisplatin (CDDP; IC50 = 8.0 μM). The toxicity against non-cancerous cell line, WI-38, was low with the IC50 > 10 μM. Treatment with this compound resulted in decreasing HPV E6 expression. Furthermore, increasing p53 and decreasing Bcl-2 expression were noted. Cell cycle profiles revealed an accumulation of cells in the G2/M phase.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Sangthong S,Sangphech N,Palaga T,Ngamrojanavanich N,Puthong S,Vilaivan T,Muangsin Ndoi
10.1016/j.ejmech.2014.02.006subject
Has Abstractpub_date
2014-04-22 00:00:00pages
334-42eissn
0223-5234issn
1768-3254pii
S0223-5234(14)00126-3journal_volume
77pub_type
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