Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Qiyu Qiu"'
Publikováno v:
Journal of Exploratory Research in Pharmacology. 7:76-84
Autor:
Bertrand J. Jean-Claude, Juozas Domarkas, Anne-Laure Larroque-Lombard, Qiyu Qiu, Suman Rao, Bernard F. Gibbs, Zakaria Rachid, Youqiang Fang, Xin Gao
Publikováno v:
The Prostate. 72:1273-1285
PURPOSE At the preclinical stage, mitozolomide (MTZ) showed exciting preclinical activity but failed later in clinical trial due to toxic side effects. We surmised that by targeting MTZ to epidermal growth factor receptor (EGFR), we may not only alte
Publikováno v:
Drug Metabolism Letters. 5:141-149
Combi-molecules are agents designed to block receptors on their own and to further degrade to bioactive agents. Here we studied the fate of a novel combi-molecule of triazene class termed “ZRS1” in biological medium using multilayer aggregates an
Autor:
Gina Belinsky, Bertrand J. Jean-Claude, Qiyu Qiu, Margarita Todorova, Meaghan MacPhee, Zakaria Rachid
Publikováno v:
Investigational New Drugs. 29:833-845
Previous strategies for stabilizing combi-triazenes were based on masking the 1,2,3-triazene chain with a 3-acetoxymethylene group. The half-lives of the latter molecules were only ca 5 min longer than those of their parent 1,2,3-triazenes. The novel
Autor:
Janet M. Hartley, Qiyu Qiu, John A Hartley, Bertrand J. Jean-Claude, Christopher Williams, Fouad Brahimi, Zakaria Rachid
Publikováno v:
Journal of Medicinal Chemistry. 50:2605-2608
To enhance the potency of "combi-molecules", we designed 6a-d and 18 to release an inhibitor of EGFR TK and a bifunctional alkylator. The combi-molecules blocked EGFR TK with potency increasing with the basicity of the mustard moiety. They selectivel
Autor:
Athanasia Katsoulas, Juozas Domarkas, Bertrand J. Jean-Claude, James P. McNamee, Qiyu Qiu, Ranjita Banerjee
Publikováno v:
Anti-Cancer Drugs. 18:171-177
We recently designed molecules termed "type II combi-molecules" to block the epidermal growth factor receptor and to damage DNA without the requirement for hydrolytic cleavage. Here, we studied two such combi-molecules (JDD36 and JDE05), containing a
Autor:
Zakaria Rachid, Nahid Golabi, Anne-Laure Larroque-Lombard, Ying Huang, Bertrand J. Jean-Claude, Fouad Brahimi, Qiyu Qiu
Publikováno v:
Journal of pharmaceutical and biomedical analysis. 56(3)
ZR2003 is a type II of combi-molecule designed to target DNA and the epidermal growth factor receptor (EGFR) without requirement for hydrolysis. In human tumour cell lines cultured as monolayers, it showed 6.5–35 fold greater activity than Iressa.
Autor:
Ying Huang, Bertrand J. Jean-Claude, Qiyu Qiu, Gina Belinsky, James P. McNamee, Ranjita Banerjee
Publikováno v:
Cellular signalling. 23(4)
RB24 (NSC 741279), a 3-methyltriazene termed “combi-molecule” designed to possess mixed epidermal growth factor receptor (EGFR) targeting and DNA methylating properties showed over a 100-fold greater antiproliferative activity than Temodal® (TEM
Autor:
Shadreck Mzengeza, Anne-Laure Larroque, Jean-Paul Soucy, Younes Lakhrissi, Qiyu Qiu, Bernard F. Gibbs, Youqiang Fang, Zakaria Rachid, Bertrand J. Jean-Claude
Publikováno v:
Drug metabolism letters. 3(1)
Combi-molecules are novel agents designed to be hydrolyzed into two bioactive species: an epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitor + a DNA alkylating agent. With the purpose of enhancing the tumour concentration of the b
Autor:
Brad Peori, Christopher Williams, Bertrand J. Jean-Claude, Anne-Laure Larroque, You Qiang Fang, Qiyu Qiu, Zakaria Rachid
Publikováno v:
Chemical biologydrug design. 71(4)
A novel type of 3,3-disubstituted bis-triazenes containing an ethylaminoethyl linker flanked by two identical anilinoquinazoline ring was synthesized. These model molecules contained an N-ethylaminomorpholine moiety designed to enhance water solubili