905449-88-9Relevant academic research and scientific papers
Preparation method of maytansine DM1 polymer
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Paragraph 0024-0055, (2021/05/26)
The invention discloses a preparation method of a maytansine DM1 polymer. The invention provides a preparation method of a compound as shown in a formula I. The preparation method comprises the following steps: DM1 is subjected to oxidation reaction as shown in the specification in a solvent to obtain the compound as shown in the formula I. The solvent is an amide solvent or a mixed solvent of the amide solvent and water. The preparation method of the compound I is simple in process, easy to operate, high in yield and low in cost.
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.
