期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 13, 页码 4830-4843出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.04.080
关键词
Pyrrolo[3,2-h]quinolinones; Angelicin heteroanalogues; Photochemotherapy; Phototoxicity
资金
- Ministero dell'Istruzione dell'Universita e della Ricerca
In the search for new photochemotherapeutic agents, a series of derivatives of the ring system pyrrolo[3,2-h]quinoline-bioisosters of the angular furocoumarin angelicin-were synthesized through a four-step synthetic approach, in reasonable overall yields. Eight of the synthesized derivatives showed a remarkable phototoxicity against a panel of four human tumor cell lines and a great dose UV-A dependence, reaching IC50 values at submicromolar level. The mode of cellular death photoinduced by pyrrolo[3,2-h]quinolines was evaluated through a series of flow cytometric analysis and other tests were performed to clarify their mechanism of action. (C) 2010 Elsevier Ltd. All rights reserved.
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