363140-31-2Relevant academic research and scientific papers
SIGMA-2 RECEPTOR LIGAND DRUG CONJUGATES AS ANTITUMOR COMPOUNDS, METHODS OF SYNTHESIS AND USES THEREOF
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Paragraph 0151-0152, (2016/01/29)
Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described. At least one described molecular species exhibits an IC50 value below 5 μΜ against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo, and led to 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
Synthesis and sigma receptor binding affinities of 8-azabicyclo[3.2.1]octan-3α-yl and 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamates
Mach,Yang,Wu,Kuhner,Whirrett,West
, p. 339 - 355 (2007/10/03)
A series of N-(8-benzyl-8-azabicyclo[3.2.1]octan-3α-yl)carbamates and N-(9-benzyl-9-azabicyclo[3.3.1]nonan-3α-yl)carbamates was prepared and their affinities for sigma (σ1 and σ2) and serotonin 5-HT3 and 5-HT4 receptors was measured in vitro. The results of this structure-activity relationship study identified a novel compound, N-(9-benzyl-9-aza-bicyclo[3.3.1]nonan-3α-yl)N′- (2-methoxy-5-methylphenyl)carbamate (4i), having a high affinity and moderate selectivity for σ2 versus σ1 receptors and a low affinity for 5-HT3 and 5-HT4 receptors. The results of this structure-activity relationship study should provide valuable information for the preparation of σ2-selective ligands that can be used to further characterize the functional role of this receptor in vivo.
