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| Dokumentenart: | Artikel | ||||
|---|---|---|---|---|---|
| Titel eines Journals oder einer Zeitschrift: | Bioorganic & medicinal chemistry letters | ||||
| Verlag: | Elsevier | ||||
| Band: | 17 | ||||
| Nummer des Zeitschriftenheftes oder des Kapitels: | 10 | ||||
| Seitenbereich: | S. 2844-2848 | ||||
| Datum: | 2007 | ||||
| Zusätzliche Informationen (Öffentlich): | 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) | ||||
| Institutionen: | Chemie und Pharmazie > Institut für Pharmazie > Lehrstuhl Pharmazeutische Biologie (Prof. Heilmann) | ||||
| Identifikationsnummer: |
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| Stichwörter / 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-Dezimal-Klassifikation: | 500 Naturwissenschaften und Mathematik > 570 Biowissenschaften, Biologie 500 Naturwissenschaften und Mathematik > 540 Chemie | ||||
| Status: | Veröffentlicht | ||||
| Begutachtet: | Ja, diese Version wurde begutachtet | ||||
| An der Universität Regensburg entstanden: | Ja | ||||
| Dokumenten-ID: | 17234 |
Zusammenfassung
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 ...
Zusammenfassung
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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