17416-87-4Relevant academic research and scientific papers
PRODRUGS OF ANTI-CANCER AND ANTI-AUTOIMMUNE DISEASES THERAPEUTIC AGENTS, AND METHODS OF MAKING AND USE THEREOF
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Paragraph 00203-00204, (2020/07/04)
The invention relates to prodrugs of anti-cancer and anti-autoimmune diseases therapeutic agents, and methods of making and use thereof.
Small molecule ligands for active targeting of TrkC-expressing tumor cells
Ko, Eunhwa,Kamkaew, Anyanee,Burgess, Kevin
supporting information, p. 1008 - 1012 (2013/02/23)
A small molecule motif was used in active targeting to deliver cytotoxic substances into tumor cells that express the TrkC receptor. Underlying this study was the hypothesis that internalization of targeted conjugates into cells would be facile if mediated by receptor binding and receptor-ligand internalization. Initial experiments using 6-mercaptopurine gave encouraging data but demonstrated the importance of maintaining solubility and high cytotoxicity. Conjugates of the targeting agent with a cytotoxic rosamine (similar to a rhodamine) were more successful. Targeting of TrkC was observed, validated in a series of competition experiments featuring other TrkC ligands, and accumulation into lysosomes was observed, as expected for receptor-mediated internalization.
TREATMENT OR PROPHYLAXIS OF PROLIFERATIVE CONDITIONS
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Page/Page column 60-61, (2010/11/17)
The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
