Pt(II) and Pd(II) derivatives of ter-butylsarcosinedithiocarbamate. Synthesis, chemical and biological characterization and in vitro nephrotoxicity.
This work reports on the synthesis, characterization and biological activity of new coordination compounds of the type [M(TSDTM)X(2)] (M=Pt(II), Pd(II); X=Cl, Br; TSDTM=ter-butylsarcosine(S-methyl)dithiocarbamate) and [Pd(TSDT)X](n) (TSDT=ter-butylsarcosinedithiocarbamate) in order to study their behavior as potential antitumor agents. All the synthesized compounds were characterized by means of elemental analysis, FT-IR, (1)H and (13)C-NMR spectroscopy and thermogravimetric analysis, suggesting a chelate S,S' structure of the TSDTM/TSDT ligand in a square-planar geometry. Finally, the synthesized complexes have been tested for in vitro cytotoxic activity against human leukemic HL60 and adenocarcinoma HeLa cells; the most active compound [Pt(TSDTM)Br(2)], characterized by IC(50) values very similar to those of the reference compound (cisplatin), was also tested for in vitro nephrotoxicity showing a very low renal cytotoxicity as compared to cisplatin itself.
Fregona
D
D
University Department of Inorganic, Metallorganic and Analytical Chemistry, via Loredan 4, 35131, Padova, Italy. dolores.fregona@unipd.it
Giovagnini
L
L
Ronconi
L
L
Marzano
C
C
Trevisan
A
A
Sitran
S
S
Biondi
B
B
Bordin
F
F
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D018922:HL-60 Cells; D006367:HeLa Cells; D006801:Humans; D007668:Kidney / Q000166:cytology / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008968:Molecular Conformation; D010165:Palladium / Q000737:chemistry*; D010984:Platinum / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012521:Sarcosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017550:Spectroscopy, Fourier Transform Infrared; D013859:Thiocarbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000970:Antineoplastic Agents; D013859:Thiocarbamates; C055171:sarcosine dithiocarbamate; D010984:Platinum; D010165:Palladium; D012521:Sarcosine