115088-06-7Relevant academic research and scientific papers
BICYCLIC PEPTIDE LIGAND STING CONJUGATES AND USES THEREOF
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Paragraph 00522, (2019/03/05)
The present invention provides compounds, compositions thereof, and methods of using the same.
METHOD FOR PREPARING ACTIVATED ESTERS
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Page/Page column 3-4, (2012/01/13)
The invention relates to a method for preparing an activated ester of the formula (I), where R is a (C1-C6) alkyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, and ALK is a (C1-C6) alkylene group, said method consisting of reacting the dicyclohexylamine P1 salt and the disuccinimidyl carbonate (DSC) in a solvent in which the dicyclohexylamine salt of the N-hydroxysuccinimide P2 is precipitated. The invention also relates to products of the formula P1.
Semisynthetic Maytansine analogues for the targeted treatment of cancer
Widdison, Wayne C.,Wilhelm, Sharon D.,Cavanagh, Emily E.,Whiteman, Kathleen R.,Leece, Barbara A.,Kovtun, Yelena,Goldmacher, Victor S.,Xie, Hongsheng,Steeves, Rita M.,Lutz, Robert J.,Zhao, Robert,Wang, Lintao,Bl?ttler, Walter A.,Chari, Ravi V. J.
, p. 4392 - 4408 (2007/10/03)
Maytansine, a highly cytotoxic natural product, failed as an anticancer agent in human clinical trials because of unacceptable systemic toxicity. The potent cell killing ability of maytansine can be used in a targeted delivery approach for the selective destruction of cancer cells. A series of new maytansinoids, bearing a disulfide or thiol substituent were synthesized. The chain length of the ester side chain and the degree of steric hindrance on the carbon atom bearing the thiol substituent were varied. Several of these maytansinoids were found to be even more potent in vitro than maytansine. The targeted delivery of these maytansinoids, using monoclonal antibodies, resulted in a high, specific killing of the targeted cells in vitro and remarkable antitumor activity in vivo.
Desmosine derivatives having a disulfide bond and preparation of artificial antigen using the same
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, (2008/06/13)
A novel desmosine derivative, which is useful for preparing a desmosine artificial antigen, has an activated, disulfide bond on the side chain at 3 or 5 position of the pyridinium ring. The derivative can combine with a polymer having thiel groups by a disulfide bond to form the effective artificial antigen.
