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| Dokumentenart: | Artikel | ||||
|---|---|---|---|---|---|
| Titel eines Journals oder einer Zeitschrift: | European journal of medicinal chemistry | ||||
| Verlag: | Elsevier | ||||
| Band: | 40 | ||||
| Nummer des Zeitschriftenheftes oder des Kapitels: | 11 | ||||
| Seitenbereich: | S. 1123-1128 | ||||
| Datum: | 2005 | ||||
| Zusätzliche Informationen (Öffentlich): | CAN 144:23119 34-3 Amino Acids, Peptides, and Proteins 636-47-5 (Distamycin A); 132244-47-4; 287734-07-0 Role: PAC (Pharmacological activity), BIOL (Biological study) (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship); 870476-34-9P; 870476-35-0P; 870476-36-1P; 870476-37-2P; 870476-38-3P; 870476-39-4P; 870476-40-7P; 870476-41-8P; 870476-42-9P Role: PAC (Pharmacological activity), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship); 207845-97-4; 245358-71-8; 561318-70-5; 870476-43-0; 870476-44-1; 870476-45-2 Role: RCT (Reactant), RACT (Reactant or reagent) (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship) | ||||
| 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 alpha -bromoacryloyl lexitropsin conjugates, their antitumor activity, and structure-activity relationship) Antitumor agents Cytotoxicity Leukemia (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their antitumor activity, and structure-activity relationship) Human (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship) bromoacryloyl lexitropsin conjugate prepn antitumor structure activity lexitropsin heterocyclic benzoheterocyclic bromoacryloyl prepn antitumor structure activity human antitumor lexitropsin bromoacryloyl structure activity | ||||
| 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: | 17226 |
Zusammenfassung
The design, synthesis and biol. evaluation of lexitropsins bearing mixed heterocyclic and benzoheterocyclic moieties and tethered to an alpha-bromo acrylic moiety acting as alkylating moiety are reported, and structure-activity relationships detd. For example, indolecarboxylic acid I reacted with pyrrole deriv. II to give analog III (X = Y = CH, Z = NMe) in 63% yield. With respect to ...
Zusammenfassung
The design, synthesis and biol. evaluation of lexitropsins bearing mixed heterocyclic and benzoheterocyclic moieties and tethered to an alpha-bromo acrylic moiety acting as alkylating moiety are reported, and structure-activity relationships detd. For example, indolecarboxylic acid I reacted with pyrrole deriv. II to give analog III (X = Y = CH, Z = NMe) in 63% yield. With respect to antiproliferative activity against L1210 and K562 cells, III (X = H, Y = CH, Z = NMe; X = CH, Y = H, Z = NMe) showed the greatest potency, while III (X = Y = CH, Z = NMe, O) exhibit the lowest activity. Among the synthesized compds. III (X = CH, Y = H, Z = NMe) was found to be the most potent member of this class and it is 70-fold more active than the bis-pyrrole counterpart against L1210 cell line. In addn., the cytotoxicity of derivs. III against KB cells and the influence of different glutathione (GSH) concns. on the cytotoxic effects was also investigated.
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