The Development of More Effective Platinum Therapy

Equilibrium Studies on Complex‐Formation Reactions of Pd[(2‐(2‐aminoethyl)pyridine)(H2O)2]2+ with Ligands of Biological Significance and Displacement Reactions of DNA Constituents

“…[2,3] In the search for new platinum anticancer drugs, great efforts are devoted to the design of complexes more efficient and less toxic than the reference drugs already in clinical use. For this purpose, the rational design of complexes and the study of relevant structure-activity relationships have been extended to families of new compounds having high structural diversity.…”

“…This is in line with the finding that cis-Pt(1,4-DACH)Cl 2 , where a seven-membered chelate ring is formed, is more active than cisplatin and oxaliplatin in several in vivo and in vitro tests. [10] For these reasons we have performed a systematic study of the complex formations of [Pd(AEP)(H 2 O) 2 ] 2+ with various biologically relevant ligands and also studied the displacement reactions of some DNA constituents bound to this complex.…”

Complex Formation and Ligand Substitution Reactions of (2-Picolylamine)palladium(II) with Various Biologically Relevant Ligands. Characterization of (2-Picolylamine)(1,1-cyclobutanedicarboxylato)palladium(II)

“…cis -Diamminedichloroplatinum(II), cisplatin, is one of the most effective agents against cancer of the chest, ovaries, bladder, head, and neck, , but severe toxicities limit its use. , In vivo cisplatin binds to DNA to form intrastrand cross-links between two neighboring guanosines, leading to distortion of DNA. , cis -Diammine(1,1-cyclobutanedicarboxylato)platinum(II), carboplatin, , the clinically successful second-generation platinum complex, does not exhibit significant nephrotoxicity compared to the first-generation antitumor drug cisplatin. This has been related to the greater pharmacokinetic stability of its 1,1-cyclobutanedicarboxylate (CBDCA) ligand in solution. , The mode of carboplatin binding to DNA is believed to be the same as that for cisplatin.…”

Síntese e atividade citotóxica de alguns azido-ciclopaladados estabilizados com ligantes bifosfínicos

“…A eficácia da cisplatina cis-[Pt(NH 3 ) 2 Cl 2 ] e da carboplatina [Pt(NH 3 ) 2 (cbdca)], (cbdca =1,1'-ciclobutanodicarboxilato) no tratamento clínico de tumores do ovário, dos testículos, da cabeça e do pescoço já é bem conhecida 1 . Entretanto existe um grande interesse no desenvolvimento de novos agentes quimioterápicos a base de metais de transição, especialmente de metais pertencentes ao grupo da platina, que sejam menos tóxicos e, ou possuam um espectro de atividade antitumoral mais amplo 2 .…”