72040-64-3Relevant articles and documents
Synthesis and tumor cell growth inhibitory activity of biotinylated annonaceous acetogenins
Shi, Jing-Fang,Wu, Ping,Jiang, Zi-Hua,Wei, Xiao-Yi
, p. 219 - 228 (2014)
Nineteen biotinylated squamocin/bullatacin derivatives have been synthesized for targeted delivery to biotin receptor overexpressed tumor cells. Most biotinylated squamocin and bullatacin derivatives show similar in vitro cytotoxicity against the biotin receptor non-overexpressed L1210 cells as squamocin and bullatacin, respectively, while against biotin receptor overexpressed 4T1 and P815 tumor cells, several derivatives show significantly higher potency and better selectivity. Among all the synthesized compounds, 15,28-di-O-(6-biotinylamidohexanoyl)squamocin (16) is the most potent, which is 10 and 26 times more active than squamocin against 4T1 and P815 cells, respectively. Compound 16 also appears to be six and fifteen times more selective than squamocin towards 4T1 and P815 cells, respectively, against L1210 cells. The structure activity relationship analysis has revealed that the preferred site for biotinylation is different for squamocin and bullatacin, and it also depends on whether a linking spacer is present.
Synthesis and in?vitro anticancer activities of biotinylated derivatives of glaucocalyxin A and oridonin
Huang, Xiao-Lei,Chen, Jing-Lei,Li, Xian-Lun,Zhao, Lei,Cui, Ya-Dong,Liu, Jiang-Yun,Morris-Natschke, Susan L.,Masuo, Goto,Cheng, Yung-Yi,Lee, Kuo-Hsiung,Chen, Dao-Feng,Zhang, Jian
, p. 703 - 711 (2020/06/03)
Fourteen glaucocalyxin A biotinylated derivatives, one glaucocalyxin C biotinylated derivative, and two oridonin biotinylated derivatives were designed and synthesized. Their structures were confirmed from 1H NMR, 13C NMR and HRMS data. The derivatives were evaluated for cytotoxic activities against lung (A549), cervical cancer cell line HeLa derivative (KB), multidrug-resistant KB subline (KB-VIN), triple-negative breast (MDA-MB-231), and estrogen receptor-positive breast (MCF-7) cancer cell lines. (Figure presented.).
BIOCONJUGATES WITH A CONTROLLED DEGREE OF CONJUGATION, THEIR PROCESS OF PREPARATION, AND THE REAGENTS FOR THEIR PREPARATION
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Page/Page column 35, (2019/01/22)
The present invention relates to a process for preparation of heterogeneous monodisperse mixtures of protein conjugates with a defined degree of conjugation (1-8) obtained by using a tri-functional reagent allowing affinity concentration followed by subse