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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Journal or Publication Title: | Bioorganic & medicinal chemistry letters | ||||
| Publisher: | Elsevier | ||||
| Volume: | 17 | ||||
| Number of Issue or Book Chapter: | 10 | ||||
| Page Range: | pp. 2844-2848 | ||||
| Date: | 2007 | ||||
| Additional Information (public): | CAN 147:95597 28-9 Heterocyclic Compounds (More Than One Hetero Atom) 942267-96-1P; 942267-97-2P; 942267-98-3P; 942267-99-4P; 942268-00-0P Role: PAC (Pharmacological activity), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (prepn. of hybrid mols. contg. benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and alpha -bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukemia cells); 109-76-2 (1,3-Diaminopropane); 124-09-4 (1,6-Diaminohexane); 196196-26-6; 207845-97-4; 245358-71-8; 294174-53-1; 561318-70-5 Role: RCT (Reactant), RACT (Reactant or reagent) (prepn. of hybrid mols. contg. benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and alpha -bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukemia cells); 942268-01-1P; 942268-02-2P Role: RCT (Reactant), SPN (Synthetic preparation), PREP (Preparation), RACT (Reactant or reagent) (prepn. of hybrid mols. contg. benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and alpha -bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukemia cells) | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) | ||||
| Identification Number: |
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| Keywords: | Structure-activity relationship (antitumor prepn. of hybrid mols. contg. benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and alpha -bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukemia cells) Antitumor agents Apoptosis Human Leukemia (prepn. of hybrid mols. contg. benzo[4,5]imidazo[1,2-d][1,2,4]thiadiazole and alpha -bromoacryloyl moieties as potent apoptosis inducers on human myeloid leukemia cells) benzoimidazothiadiazole bromoacryloyl prepn apoptosis inducer myeloid leukemia | ||||
| Dewey Decimal Classification: | 500 Science > 570 Life sciences 500 Science > 540 Chemistry & allied sciences | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 17234 |
Abstract
The synthesis and biol. activity of a series of hybrids I (n = 3, 6; X = NH, NMe, O, S) prepd. 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 compds. were highly cytotoxic against the human myeloid leukemia cell lines HL-60 and ...
Abstract
The synthesis and biol. activity of a series of hybrids I (n = 3, 6; X = NH, NMe, O, S) prepd. 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 compds. were highly cytotoxic against the human myeloid leukemia cell lines HL-60 and U937 (IC50 0.24-1.72 micro M), significantly superior to that of both alkylating units alone. In human myeloid leukemia HL-60 cells we obsd. that these compds. suppress survival and proliferation by triggering morphol. changes and internucleosomal DNA fragmentation characteristic of apoptotic cell death. The apoptosis induced by these compds. is mediated by caspase-3 activation and is also assocd. to an early release of cytochrome c from the mitochondria.
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