Cellular Pharmacology of the Novel Antitumoural Cyanoguanidine CHS 828
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Multiparametric evaluation of apoptosis: effects of standard cytotoxic agents and the cyanoguanidine CHS 828.
A multiparametric high-content screening assay for measurement of apoptosis was developed. HeLa cells and lymphoma U-937 cells were exposed to cytotoxic drugs in flat-bottomed optical microtiter plates. After incubation, the DNA-binding dye Hoechst 33342, fluorescein-tagged probes that covalently bind active caspases and chloromethyl-X-rosamine to detect mitochondrial membrane potential (MMP) w...
متن کاملCHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo.
A new class of recently discovered antineoplastic agents, the pyridyl cyanoguanidines, exert a potent antitumor activity in rodents after oral administration. Optimization in vitro and in vivo has resulted in the selection of the lead candidate CHS 828 (N-(6-chlorophenoxyhexyl)-N'cyano-N"-4-pyridylguanidine). CHS 828 was found to exert potent cytotoxic effects in human breast and lung cancer ce...
متن کاملPharmacological Studies of CHS 828 and Etoposide Induced Tumour Cell Death
Martinsson, P. 2001. Pharmacological studies of CHS 828 and etoposide induced tumour cell death. Acta Universitatis Upsaliensis. Comprehensive Summaries of Uppsala Dissertations from the Faculty of Medicine 1095. 53 pp. Uppsala. ISBN 91554-5157-8. Antitumour properties of the cyanoguanidine CHS 828 and analogues were discovered in 1997. CHS 828 is presently in clinical phase I/II trials. This t...
متن کاملA Phase I study of CHS 828 in patients with solid tumor malignancy.
CHS 828 is a cyanoguanidine, which has demonstrated potent antitumor activity in preclinical tumor models. The activity of CHS 828 in vitro showed only low to moderate correlation to other antineoplastic agents suggesting a unique mechanism of action. Ten females and 6 males (median age 58 years) with solid tumors refractory to standard therapy were included in this Phase I study. The study dru...
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Cyanoguanidines as well as azoles are important bioactive groups, which play an important role in the medical application; meanwhile, the high nitrogen content makes them excellent backbones for energetic materials. A Novel and simple method that combined these two fragments into one molecular compound was developed through the transformation of dicyanamide ionic salts. In return, compounds 4-1...
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