The development of effective and selective anticancer agents remains a critical challenge in modern medicine. This study presents the synthesis and characterization of two novel dyads, AuP-SnPh2 and AuP-Sn2Ph6, formed by covalently linking a cationic gold porphyrin to organotin(IV) malonate complexes. These compounds were designed to investigate whether combining gold porphyrin with tin-based organometallic entities could generate synergistic cytotoxic effects against cancer cells while maintaining selectivity over healthy tissues. The first dyad features a single tin(IV) center coordinated through a malonate linker and two phenyl groups (SnPh2), whereas the second incorporates two tin(IV) centers each bound to one carboxylic acid group of the malonate and three phenyl ligands (SnPh3), forming a dinuclear structure.
Structural analysis using IR spectroscopy and 119Sn NMR revealed that in the solid state, both complexes adopt a polymeric coordination network with penta-coordinated tin atoms bridging two malonate units.Phospho-ULK1(Ser757) Antibody Epigenetics In solution, however, the 119Sn NMR signals indicated monomeric species with tetrahedral geometry, suggesting dissociation from the polymer upon solvation. UV-Vis absorption spectra confirmed the dominance of gold porphyrin transitions, with no significant electronic interaction between the porphyrin and tin moieties, consistent with the presence of a non-conjugated methylene spacer.Streptolysin O Antibody In stock
Biological evaluation demonstrated that both dyads exhibit significantly enhanced cytotoxicity compared to equimolar mixtures of their individual components—gold porphyrin and reference tin complexes.PMID:34614295 Notably, AuP-SnPh2 displayed potent activity against MCF-7 breast cancer cells (LC50 = 0.13 µM) with a favorable selectivity index, as it was less toxic to healthy fibroblasts (LC50 = 0.41 µM). In contrast, AuP-Sn2Ph6 showed even greater potency (LC50 = 0.024 µM on cancer cells), but its toxicity extended to healthy cells (LC50 = 0.032 µM), reducing its therapeutic window. Mechanistic studies revealed that both dyads induce cell cycle arrest at the G0/G1 phase without triggering apoptosis or disrupting cytoskeletal integrity, suggesting a unique mode of action involving quiescence induction rather than direct cell death pathways.
These findings highlight the potential of integrating gold porphyrins with organotin systems to develop metallo-drugs with amplified anticancer activity. While AuP-SnPh2 emerges as a promising candidate due to its balance of potency and selectivity, further optimization is needed for the highly active but non-selective AuP-Sn2Ph6. Overall, this work establishes a foundation for designing next-generation metallodrugs targeting cell cycle regulation in cancer therapy.MedChemExpress (MCE) offers a wide range of high-quality research chemicals and biochemicals (novel life-science reagents, reference compounds and natural compounds) for scientific use. We have professionally experienced and friendly staff to meet your needs. We are a competent and trustworthy partner for your research and scientific projects.Related websites: https://www.medchemexpress.com