Characterization of novel nitroplatinum(iv) complexes for the treatment of cancer

摘要: Many types of chemotherapeutic agents have been developed to target specific mechanisms within the body that control progression cancer, though few able circumvent existing problems associated with treatments. The current remedies entail grueling drug regimens and toxic side effects may undermine effectiveness drugs. Cisplatin, a common nitroplatinum(II) widely used treat variety cancers, is administered intravenously circulates systemically, affecting healthy regions as well. Resistance cisplatin increasing need for new, less medication must be met future success in cancer therapy. Our lab has synthesized novel nitroplatinum(IV) complexes (PH1-14) evade these problems. We examined compounds on cell viability, well cancer-specific such nitric oxide (NO) production, angiogenesis, STAT signaling pathways. In vitro studies demonstrated PH111 PH14 greater efficacy at inhibiting proliferation lower IC50 values ranged from 41-58 uM (as compared = 66 uM). Data NO assays were inconclusive, there was elevated expression inducible synthase cells treated PH3 PH11. also found PH9 inhibit dimerization concentrations low 0.3 uM. decreased VEGF HIF-1α expression, thereby angiogenesis. activity