Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A New Class of Agents with High Apoptotic Activity in Chronic Myelogenous Leukemia K562 Cells and in Cells from Patients at Onset and Who Were
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- 作者：Romano Silvestri ; Gabriella Marfè ; Marino Artico ; Giuseppe La Regina ; Antonio Lavecchia ; Ettore Novellino ; Manuela Morgante ; Carla Di Stefano ; Gianfranco Catalano ; Giuseppe Filomeni ; Elisabett
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：September 21, 2006
- 年：2006
- 卷：49
- 期：19
- 页码：5840 - 5844
- 全文大小：110K
- 年卷期：v.49,no.19(September 21, 2006)
- ISSN：1520-4804
文摘
Pyrrolo[1,2-b][1,2,5]benzothiadiazepine 5,5-dioxides (PBTDs) induced apoptosis in human BCR-ABL-expressing leukemia cells. The apoptotic activity was also observed in primary leukemic blasts, obtainedfrom chronic myelogenous leukemia (CML) patients at onset or from patients in blast crisis and who wereimatinib-resistant. Compounds 5 and 14 induced apoptosis before BCR-ABL protein expression and tyrosinphosphorylation were affected and activated different caspases in the apoptotic pathway. PBTDs are a newclass of valid candidates for the treatment of CML.