title: Cytotoxic and proapoptotic effects of new Pd(II) and Pt(II)-complexes with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphosphinin-4-ol-2-oxide.
abstract: The new palladium (II) and platinum (II) complexes 2 and 3 with 3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphospinin-4-ol-2-oxide 1 were synthesized and their physicochemical and pharmacological properties were determined. The cytotoxic effects of these complexes were examined on the two human leukemia cell lines, HL-60 and NALM-6. Pd-complex 2 and Pt-complex 3 exerted significant cytotoxic activity. The effects exhibited by these two complexes were comparable to those reported for cis-platin and carboplatin. On the other hand, ligand 1 was not cytotoxic. As determined by caspase-3 activity assay, compounds 2 and 3 differed slightly in their mode of induction of the programmed cell death.
authors.affiliation: Department of Bioorganic Chemistry, Medical University, Muszyńskiego 1, PL 90-151 Łódź, Poland. elora@ich.pharm.am.lodz.pl
authors.forename: Elzbieta
authors.initials: E
authors.lastname: Budzisz
authors.forename: Urszula
authors.initials: U
authors.lastname: Krajewska
authors.forename: Marek
authors.initials: M
authors.lastname: Rózalski
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3; D020169:Caspases / Q000378:metabolism; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004790:Enzyme Induction; D006801:Humans; D007094:Imides / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000737:chemistry / Q000494:pharmacology*; D009943:Organophosphorus Compounds / Q000737:chemistry / Q000494:pharmacology*; D009944:Organoplatinum Compounds / Q000737:chemistry / Q000494:pharmacology; D010165:Palladium; D010984:Platinum; D013997:Time Factors
chemical_list: C500345:3-ethanimidoyl-2-methoxy-2H-1,2-benzoxaphospinin-4-ol-2-oxide; D000970:Antineoplastic Agents; D007094:Imides; D009942:Organometallic Compounds; D009943:Organophosphorus Compounds; D009944:Organoplatinum Compounds; D010984:Platinum; D010165:Palladium; C505407:CASP3 protein, human; D053148:Caspase 3; D020169:Caspases