title: Antiproliferative and erythroid differentiation of piperazine and triphenyl derivatives against k-562 human chronic myelogenous leukemia.
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 erythroid 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 μg 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.
authors.affiliation: Chemistry Department, Faculty of Sciences II, Lebanese University, Fanar, Beirut, Lebanon. antsaab@gmail.com
authors.forename: Antoine Michael
authors.initials: AM
authors.lastname: Saab
authors.forename: Michael
authors.initials: M
authors.lastname: Dobmeier
authors.forename: Burkhard
authors.initials: B
authors.lastname: Koenig
authors.forename: Enrica
authors.initials: E
authors.lastname: Fabri
authors.forename: Alessia
authors.initials: A
authors.lastname: Finotti
authors.forename: Monica
authors.initials: M
authors.lastname: Borgatti
authors.forename: Ilaria
authors.initials: I
authors.lastname: Lampronti
authors.forename: Francesco
authors.initials: F
authors.lastname: Bernardi
authors.forename: Thomas
authors.initials: T
authors.lastname: Efferth
authors.forename: Roberto
authors.initials: R
authors.lastname: Gambari
mesh_terms: D016923:Cell Death / Q000187:drug effects; D002454:Cell Differentiation / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D041905:Erythroid Cells / Q000187:drug effects / Q000378:metabolism / Q000473:pathology; D006801:Humans; D020014:K562 Cells; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000473:pathology*; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D008926:Plicamycin / Q000494:pharmacology; D013730:Terphenyl Compounds / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D010879:Piperazines; D013730:Terphenyl Compounds; D000077489:Piperazine; D008926:Plicamycin
keywords: Antiproliferative activity; anticancer agents; erythroid differentiation; piperazine derivatives; triphenyl derivatives