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 Imatinib-Resistant

Journal of Medicinal Chemistry
2006.0

Abstract

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, obtained from chronic myelogenous leukemia (CML) patients at onset or from patients in blast crisis and who were imatinib-resistant. Compounds 5 and 14 induced apoptosis before BCR-ABL protein expression and tyrosin phosphorylation were affected and activated different caspases in the apoptotic pathway. PBTDs are a new class of valid candidates for the treatment of CML.

Knowledge Graph

Similar Paper

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 Imatinib-Resistant
Journal of Medicinal Chemistry 2006.0
Synthesis and biological evaluation of anilino substituted pyrimidine linked pyrrolobenzodiazepines as potential anticancer agents
Bioorganic & Medicinal Chemistry Letters 2010.0
Hybrids of privileged structures benzothiazoles and pyrrolo[2,1-c] [1,4]benzodiazepin-5-one, and diversity-oriented synthesis of benzothiazoles
European Journal of Medicinal Chemistry 2012.0
2-Anilinonicotinyl linked 2-aminobenzothiazoles and [1,2,4]triazolo[1,5-b] [1,2,4]benzothiadiazine conjugates as potential mitochondrial apoptotic inducers
Bioorganic & Medicinal Chemistry 2011.0
Synthesis and induction of G0–G1 phase arrest with apoptosis of 3,5-dimethyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazepin-4(3H)-one
European Journal of Medicinal Chemistry 2008.0
Synthesis of imidazothiadiazole–benzimidazole conjugates as mitochondrial apoptosis inducers
Med. Chem. Commun. 2014.0
Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents
Bioorganic & Medicinal Chemistry Letters 2008.0
Inhibitors of Apoptosis in Lymphocytes:  Synthesis and Biological Evaluation of Compounds Related to Pifithrin-α
Journal of Medicinal Chemistry 2005.0
Benzylidene thiazolidinediones: Synthesis, in vitro investigations of antiproliferative mechanisms and in vivo efficacy determination in combination with Imatinib
Bioorganic & Medicinal Chemistry Letters 2020.0
Synthesis, anticancer activity and apoptosis inducing ability of bisindole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates
Bioorganic & Medicinal Chemistry Letters 2012.0