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Dalton Trans ; 49(20): 6842-6853, 2020 May 26.
Article in English | MEDLINE | ID: mdl-32377663

ABSTRACT

In continuation of the structure-activity study about 4-substituted chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(iii) complexes as necroptosis and ferroptosis inducers, we introduced a 4-COOH group at the 1,2-phenylenediamine moiety of the lead ([Fe(iii)salopheneCl]) and derived the resulting complex 15 to the respective ethyl, propyl, or butyl amides (16-18) and esters (19-21). The compounds 16-21 exerted concentration-dependent antiproliferative and antimetabolic effects against HL-60 cells. The esters were more active than the analogous amides. Elongation of the alkyl chain enhanced the activity of the amides, while that of the esters decreased. The complexes 16-21 induced necroptosis and/or ferroptosis but not apoptosis. Studies on protein binding and uptake into HL-60 cells indicated that the complexes mainly accumulated by passive transport. The high binding tendency of all complexes to apo-Transferrin, however, points to participation of a carrier-mediated transport into the cells, too.


Subject(s)
Amides/pharmacology , Antineoplastic Agents/pharmacology , Esters/pharmacology , Ferroptosis/drug effects , Necroptosis/drug effects , Amides/chemical synthesis , Amides/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Esters/chemical synthesis , Esters/chemistry , HL-60 Cells , Humans , Molecular Structure , Structure-Activity Relationship , Tumor Cells, Cultured
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