903499-49-0Relevant academic research and scientific papers
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 and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors
Huang, Wenwei,Huang, Ruili,Attene-Ramos, Matias S.,Sakamuru, Srilatha,Englund, Erika E.,Inglese, James,Austin, Christopher P.,Xia, Menghang
, p. 5239 - 5243 (2011/10/02)
Quinazolin-4-one 1 was identified as an inhibitor of the HIF-1α transcriptional factor from a high-throughput screen. HIF-1α up-regulation is common in many cancer cells. In this Letter, we describe an efficient one-pot sequential reaction for the synthes
ERASTIN AND ERASTIN BINDING PROTEINS, AND USES THEREOF
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Page/Page column 131, (2008/06/13)
The invention relates to methods of screening for binding partners, especially binding partners essential for the biological activity of erastin (e.g. VDACs such as VDAC3). The invention also provides reagents and methods for effective killing of cancer c
