Platinum(terpyridine) complexes with N-heterocyclic carbene co-ligands: high antiproliferative activity and low toxicityin vivo

Abstract

Pt(terpyridine) complexes are well-known as DNA intercalators. The introduction of an NHC co-ligand rendered the complex highly antiproliferative in cancer cells compared to its chlorido derivative. Despite the high potency,...

Synthesis and anticancer mechanisms of four novel platinum(ii) 4′-substituted-2,2′:6′,2′′-terpyridine complexes

“…The Pt–Cl bond length (2.291(3)–2.305(3) Å) in tpy1Pt was different from those in tpy2Pt–tpy4Pt and other Pt( ii )–terpyridyl complexes. 30–42,44 The Cambridge Crystallographic Data Centre (CCDC) numbers for PtS and tpy1Pt–tpy4Pt were †…”

“…A series of coordination compounds based on terpyridyl and metals, such as copper( ii ), ruthenium( ii ), zinc( ii ), iridium( iii ), and rhenium( i ), 23–29 have been designed as antitumor drugs. 23–29 Among these, several Pt( ii )–terpyridyl complexes have been developed as important topoisomerase I/II inhibitors, 30 G-quadruplex DNA binders, 31 telomerase inhibitors, 32 DNA synthesis inhibitors, 33,34 reactive oxygen species (ROS) activators, 35 adenosine triphosphate (ATP) inhibitors, 36 mitochondrion-targeted agents, 37 photodynamic therapy agents, 38 autophagy–lysosomal system inductors, 39 and others drugs. 40–42 Nevertheless, the development of Pt( ii ) 4′-substituted-2,2′:6′,2′′-terpyridine (tpy1–tpy4) chemotherapeutics with mitophagy-targeting properties remains unexplored.…”

Investigating the Anticancer Properties of Novel Functionalized Platinum(II)–Terpyridine Complexes

“…In this context, a large and growing family of platinum(II) complexes of 2,2 ′ :6 ′ ,6 ′′terpyridine (tpy) derivatives have been receiving increased attention [1,[6][7][8].…”

“…Their fused aromatic structure makes them suitable ligands for various transition metals. The resultant complexes have been thoroughly investigated for their biological activity and physicochemical features [6,7,9]. Some diverse platinum(II) derivatives of tpy and its analogs have shown potent antiproliferative properties in vitro against several cancer cell lines, comparable to or even better than cisplatin [10,11].…”

“…The family of terpyridine-platinum complexes offers different mechanisms of action involving diverse targets. Mainly, they have been developed as important topoisomerase I/II inhibitors [9,22], G-quadruplex DNA binders [23,24], telomerase inhibitors [25,26], DNA synthesis inhibitors [6,27,28], reactive oxygen species (ROS) activators [29], adenosine triphosphate (ATP) inhibitors [30], mitochondrion-targeted agents [31], photodynamic therapy agents [32], autophagy-lysosomal system inductors [33] and modulators of βamyloid aggregation [34].…”