573698-75-6Relevant academic research and scientific papers
Enzymatically Activated Glyco-Prodrugs of Doxorubicin Synthesized by a Catalysis-Free Diels-Alder Reaction
Bliman, David,Demeunynck, Martine,Leblond, Pierre,Meignan, Samuel,Baussane, Isabelle,Fort, Sebastien
, p. 2370 - 2381 (2018)
The severe side effects associated with the use of anthracycline anticancer agents continues to limit their use. Herein we describe the synthesis and preliminary biological evaluation of three enzymatically activatable doxorubicin-oligosaccharide prodrugs. The synthetic protocol allows late stage variation of the carbohydrate and is compatible with the use of disaccharides such as lactose as well as more complex oligosaccharides such as xyloglucan oligomers. The enzymatic release of doxorubicin from the prodrugs by both protease (plasmin) and human carboxylesterases (hCE1 and 2) was demonstrated in vitro and the cytotoxic effect of the prodrugs was assayed on MCF-7 breast cancer cells.
Long-Acting Tumor-Activated Prodrug of a TGFβR Inhibitor
Augustine-Rauch, Karen,Borzilleri, Robert,Donnell, Andrew F.,Hou, Xiaoping,Huang, Audris,Kempson, James,Lombardo, Louis J.,Luk, Emily,Murtaza, Anwar,Parrish, Karen E.,Pawluczyk, Joseph,Poss, Michael A.,Purandare, Ashok V.,Raghavan, Nimmi,Smalley, James,Swanson, Jesse,Tortolani, David R.,Wan, Honghe,Yang, Zheng,Yip, Shiuhang,Zhang, Yong
, p. 15787 - 15798 (2021/11/16)
Inhibition of TGFβ signaling in concert with a checkpoint blockade has been shown to provide improved and durable antitumor immune response in mouse models. However, on-target adverse cardiovascular effects have limited the clinical use of TGFβ receptor (
New effector conjugates, process for their production and their pharmaceutical use
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Page/Page column 15-16, (2008/06/13)
Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of conjugates for treating proliferative or angiogenesis-associated processes is described.
