Romagnoli, R. and Baraldi, Pier Giovanni and Iaconinoto, M. A. and Carrion, M. D. and Tabrizi, M. A. and Gambari, R. and Borgatti, M. and Heilmann, Joerg (2005) Synthesis and biological activity of alpha-bromoacryloyl lexitropsin conjugates. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 40 (11). pp. 1123-1128. ISSN 0223-5234, 1768-3254
Full text not available from this repository. (Request a copy)Abstract
The design, synthesis and biological 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 determined. With respect to anti proliferative activity against L1210 and K562 cells, compounds 7 and 10 showed the greatest potency, while compounds 4 and 5 exhibit the lowest activity. Among the synthesized compounds 4-12, the derivative 10 was found to be the most potent member of this class and it is 70-fold more active than the bis-pyrrole counterpart 3 against L1210 cell line. In addition, the cytotoxicity of derivatives 5-12 against KB cells and the influence of different glutathione (GSH) concentrations on the cytotoxic effects was also investigated. (c) 2005 Elsevier SAS. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | LOW-MOLECULAR-WEIGHT; DNA-BINDING; DISTAMYCIN-A; BENZOHETEROCYCLIC DERIVATIVES; HALOGENOACRYLIC DERIVATIVES; ANTITUMOR-ACTIVITY; CYTOTOXICITY; CONGENERS; ANALOGS; AGENTS; glutathione; benzoheterocycle; alpha-bromoacryloyl; DNA minor groove binders |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 23 Apr 2021 10:19 |
| Last Modified: | 23 Apr 2021 10:19 |
| URI: | https://pred.uni-regensburg.de/id/eprint/35463 |
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