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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Garelnabi, Elrashied A. E. Pletsas, Dimitrios Li, Li Kiakos, Konstantinos Karodia, Nazira Hartley, John A. Phillips, Roger M. Wheelhouse, Richard T. |
| Description | Country affiliation: United kingdom Author Affiliation: Garelnabi EA ( School of Pharmacy, Institute of Cancer Therapeutics, and Chemical and Forensic Sciences, University of Bradford , Bradford BD7 1DP, U.K.); Pletsas D ( School of Pharmacy, Institute of Cancer Therapeutics, and Chemical and Forensic Sciences, University of Bradford , Bradford BD7 1DP, U.K.); Li L ( School of Pharmacy, Institute of Cancer Therapeutics, and Chemical and Forensic Sciences, University of Bradford , Bradford BD7 1DP, U.K.); Kiakos K ( UCL Cancer Institute , Paul O'Gorman Building, 72 Huntley Street, London WC1E 6BT, U.K.); Karodia N ( School of Pharmacy, Institute of Cancer Therapeutics, and Chemical and Forensic Sciences, University of Bradford , Bradford BD7 1DP, U.K.); Hartley JA ( UCL Cancer Institute , Paul O'Gorman Building, 72 Huntley Street, London WC1E 6BT, U.K.); Phillips RM ( School of Pharmacy, Institute of Cancer Therapeutics, and Chemical and Forensic Sciences, University of Bradford , Bradford BD7 1DP, U.K.); Wheelhouse RT ( School of Pharmacy, Institute of Cancer Therapeutics, and Chemical and Forensic Sciences, University of Bradford , Bradford BD7 1DP, U.K.) |
| Abstract | The imidazotetrazine ring is an acid-stable precursor and prodrug of highly reactive alkyl diazonium ions. We have shown that this reactivity can be managed productively in an aqueous system for the generation of aziridinium ions with 96% efficiency. The new compounds are potent DNA alkylators and have antitumor activity independent of the O6-methylguanine-DNA methyltransferase and DNA mismatch repair constraints that limit the use of Temozolomide. |
| File Format | HTM / HTML |
| e-ISSN | 19485875 |
| DOI | 10.1021/ml300132t |
| Journal | ACS Medicinal Chemistry Letters |
| Issue Number | 12 |
| Volume Number | 3 |
| Language | English |
| Publisher | American Chemical Society |
| Publisher Date | 2012-12-13 |
| Publisher Place | United States |
| Access Restriction | Open |
| Subject Keyword | Discipline Chemistry |
| Content Type | Text |
| Resource Type | Article |
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