Abstract:
:The cytotoxicity and photo-enhanced cytotoxicity of a series of 18 3,6-di-substituted acridines were evaluated on both tumour CHO cells and human normal keratinocytes, and compared to their corresponding clastogenicity as assessed by the micronucleus assay. Compounds 2f tert-butyl N-[(6-tert-butoxycarbonylamino)acridin-3-yl]carbamate and 2d N-[6-(pivalamino)acridin-3-yl]pivalamide displayed a specific cytotoxicity on CHO cells. These results suggested that the two derivatives could be considered as interesting candidates for anticancer chemotherapy and hypothesized that the presence of 1,1-dimethylethyl substituents was responsible for a strong nonclastogenic cytotoxicity. Compounds 2b and 2c, on the contrary, displayed a strong clastogenicity. They indicated that the presence of nonbranched aliphatic chains on positions 3 and 6 of the acridine rings tended to induce a significant clastogenic effect. Finally, they established that most of the acridine compounds could be photo-activated by UVA-visible rays and focussed on the significant role of light irradiation on their biological properties.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Benchabane Y,Di Giorgio C,Boyer G,Sabatier AS,Allegro D,Peyrot V,De Méo Mdoi
10.1016/j.ejmech.2009.01.010subject
Has Abstractpub_date
2009-06-01 00:00:00pages
2459-67issue
6eissn
0223-5234issn
1768-3254pii
S0223-5234(09)00016-6journal_volume
44pub_type
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