Romagnoli, Romeo and Baraldi, Pier Giovanni and Carrion, Maria Dora and Cruz-Lopez, Olga and Preti, Delia and Tabrizi, Mojgan Aghazadeh and Fruttarolo, Francesca and Hellmann, Joerg and Bermejo, Jaime and Estevez, Francisco (2007) Hybrid molecules containing benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and alpha-bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukaemia cells. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 17 (10). pp. 2844-2848. ISSN 0960-894X, 1464-3405
Full text not available from this repository. (Request a copy)Abstract
The synthesis and biological activity of a series of hybrids 1-5 prepared combining a benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and different benzoheterocyclic alpha-bromoacryloyl amides have been described and their structure-activity relationships discussed. All these hetero-bifunctional compounds were highly cytotoxic against the human myeloid leukaemia cell lines HL-60 and U937 (IC50 0.24-1.72 mu M), significantly superior to that of both alkylating units alone. In human myeloid leukaemia HL-60 cells we observed that these compounds suppress survival and proliferation by triggering morphological changes and internucleosomal DNA fragmentation characteristic of apoptotic cell death. The apoptosis induced by these compounds is mediated by caspase-3 activation and is also associated to an early release of cytochrome c from the mitochondria. (c) 2007 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | BENZOHETEROCYCLIC DERIVATIVES; ANTICANCER DRUGS; DEATH; 1,2,4-THIADIAZOLES; DISTAMYCIN; INHIBITION; CHEMISTRY; SPONGES; BINDING; HL-60; hybrid; apoptosis; leukaemia; antiproliferative activity |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 09 Dec 2020 15:00 |
| Last Modified: | 09 Dec 2020 15:00 |
| URI: | https://pred.uni-regensburg.de/id/eprint/32761 |
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