371226-28-7Relevant articles and documents
SIGMA-2 RECEPTOR LIGAND DRUG CONJUGATES AS ANTITUMOR COMPOUNDS, METHODS OF SYNTHESIS AND USES THEREOF
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, (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 of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs as sigma-2 receptor ligands
Mach, Robert H.,Vangveravong, Suwanna,Huang, Yunsheng,Yang, Biao,Blair, Joseph B.,Wu, Li
, p. 380 - 398 (2007/10/03)
Aseries of N-substituted-9-azabicyclo[3.3.1]nonan-3α-yl)carbamate analogs was prepared and their affinities for sigma (σ1 and σ2) receptors was measured in vitro. The results of this structure-activity relationship study identified a