Antiproliferative and Erythroid Differentiation of Piperazine and Triphenyl Derivatives Against K-562 Human Chronic Myelogenous Leukemia

Saab, Antoine Michael and Dobmeier, Michael and Koenig, Burkhard and Fabri, Enrica and Finotti, Alessia and Borgatti, Monica and Lampronti, Maria and Bernardi, Francesco and Efferth, Thomas and Gambari, Roberto (2013) Antiproliferative and Erythroid Differentiation of Piperazine and Triphenyl Derivatives Against K-562 Human Chronic Myelogenous Leukemia. ANTICANCER RESEARCH, 33 (8). pp. 3027-3032. ISSN 0250-7005, 1791-7530

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Abstract

Five piperazine derivatives (S)-4-benzyl-1-(4-bromo-3-methylphenyl)-2 methylpiperazine (A), (S)-1-benzyl-3-isobutylpiperazine-2,5-dione (B), (S)-1-benzyl-3 methylpiperazine-2,5-dione (C), (S)-1,3-dibenzylpiperazine-2,5-dione (D), (E)-1-(3-methyl 4((E)-3-(2-methylpropylidene) piperazin-1-yl) phenyl)-2-(2 methylpropylidene) piperazine (E) and triphenyl derivative ammonium 2-((2,3',3 ''-trimethyl-[1,1':4',1 '' terphenyl]-4 yl)oxy)acetate (F) were tested for inhibition of K-562 cell proliferation and for induction of etythroid differentiation. Among them, two piperazine and one triphenyl derivatives, compounds A, E, and F inhibited the proliferation of the K562 cell lines exhibiting inhibition concentration 50 (IC50) (IC50) of values 30.10+/-1.6, 4.60+/-0.4 and 25.70+/-1.10 mu g ml(-1), respectively. If compound A and F were added to suboptimal concentrations of the established anticancer drugs cytosine arabinoside or mithramycin, pronounced synergic effects were observed.

Item Type: Article
Uncontrolled Keywords: BREAST-CANCER; K562 CELLS; TAMOXIFEN; PROLIFERATION; PREVENTION; INDUCTION; LINES; ACID; Antiproliferative activity; piperazine derivatives; triphenyl derivatives; erythroid differentiation; anticancer agents
Subjects: 500 Science > 540 Chemistry & allied sciences
Divisions: Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König
Depositing User: Dr. Gernot Deinzer
Date Deposited: 03 Apr 2020 13:46
Last Modified: 03 Apr 2020 13:46
URI: https://pred.uni-regensburg.de/id/eprint/16295

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