1242062-15-2Relevant academic research and scientific papers
Bioreductively Activatable Prodrug Conjugates of Combretastatin A-1 and Combretastatin A-4 as Anticancer Agents Targeted toward Tumor-Associated Hypoxia
Chaplin, David J.,Davis, Peter,Devkota, Laxman,Gerberich, Jeni L.,Hamel, Ernest,Kuch, Bunnarack,Macdonough, Matthew T.,Mason, Ralph P.,Mondal, Deboprosad,Pinney, Kevin G.,Ramirez, Alejandro J.,Shi, Zhe,Strecker, Tracy E.,Trawick, Mary Lynn,Wang, Yifan,Winn, Blake A.
, (2020/03/30)
The natural products combretastatin A-1 (CA1) and combretastatin A-4 (CA4) function as potent inhibitors of tubulin polymerization and as selective vascular disrupting agents (VDAs) in tumors. Bioreductively activatable prodrug conjugates (BAPCs) can enha
Regio-and stereospecific synthesis of mono-β-d-glucuronic acid derivatives of combretastatin A-1
Tanpure, Rajendra P.,Strecker, Tracy E.,Chaplin, David J.,Siim, Bronwyn G.,Trawick, Mary Lynn,Pinney, Kevin G.
supporting information; experimental part, p. 1093 - 1101 (2010/09/09)
Synthetic routes have been established for the preparation of regio-and stereoisomerically pure samples of the mono-β-d-glucuronic acid derivatives of combretastatin A-1, referred to as CA1G1 (5a) and CA1G2 (6a). Judicious choice of protecting groups for the catechol ring was required for the regiospecific introduction of the glucuronic acid moiety. The tosyl group proved advantageous in this regard. The two monoglucuronic acid analogues demonstrate low cytotoxicity (compared to CA1, 2) against selected human cancer cell lines, with CA1G1 being slightly more potent than CA1G2.
