sulfinosine

Sulfinosine is a synthetic purine nucleoside analog structurally related to 6-thioguanosine that has been investigated preclinically as an antineoplastic agent, particularly in multidrug-resistant non-small cell lung cancer and glioblastoma models. It is metabolically activated via intracellular purine salvage pathways to thioguanine nucleotide analogs that disrupt DNA and RNA synthesis, leading to growth inhibition, caspase-dependent apoptosis, and autophagy in cancer cells, while exhibiting relatively low toxicity toward normal cells at active concentrations.[2] Sulfinosine also modulates multiple resistance- and progression-associated mechanisms, including depletion of glutathione, inhibition of P‑glycoprotein–mediated drug efflux with functional reversal of doxorubicin resistance, and downregulation and reduced secretion of vascular endothelial growth factor, thereby impairing angiogenic signaling.[2] Mouse chemotherapeutic characterization studies indicate favorable antitumor activity, good central nervous system penetration relative to 6‑thioguanosine, and a toxicity profile that has supported its consideration for combination regimens, although it has not progressed to broad clinical development.[2][8][10]

Other names

SF2-amino-9-beta-D-ribofuranosyl-6-mercaptopurine-5'-sulfoxide2-amino-9-β-D-ribofuranosyl-6-mercaptopurine-5'-sulfoxide