Synthesis and photochemotherapeutic activity of thiopyrano[2,3-e]indol-2-ones

被引:16
作者
Barraja, P
Sciabica, L
Diana, P
Lauria, A
Montalbano, A
Almerico, AM
Dattolo, G
Cirrincione, G
Disarò, S
Basso, G
Viola, G
Dall'Acqua, F
机构
[1] Univ Palermo, Dipartimento Fharmacochim Tossicol & Biol, I-90123 Palermo, Italy
[2] Univ Padua, Dipartimento Pediat, I-35131 Padua, Italy
[3] Univ Padua, Dipartimento Sci Farmaceut, I-35131 Padua, Italy
关键词
thiopyrano-indoles; photochemotherapeutic activity; apoptosis induction;
D O I
10.1016/j.bmcl.2005.03.016
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of derivatives of the new ring system thiopyrano[2,3-e]indol-2-one was prepared with the aim of obtaining new photochemotherapeutic drugs. Biological screenings were performed on this new class of photoactivable drugs and a strong anti-proliferative effect was observed upon irradiation with UVA light. The compound bearing a methyl substituent at the pyrrole nitrogen resulted as the most interesting showing IC50 in the nanomolar range. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2291 / 2294
页数:4
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