880649-00-3Relevant academic research and scientific papers
Design, synthesis and antiproliferative effect of 17β-amide derivatives of 2-methoxyestradiol and their studies on pharmacokinetics
Shi, Xiufang,Wang, Zhihao,Xu, Feng,Lu, Xiang,Yao, Haifeng,Wu, Dandan,Sun, Shuaijun,Nie, Ruifang,Gao, Shuo,Li, Panpan,Xia, Liwen,Zhang, Zhenzhong,Wang, Cong
, p. 6 - 14 (2017/10/27)
A series of 17β-amide-2-methoxyestradiol compounds were synthesized with an aim to enhance the antiproliferative effect of 2-methoxyestradiol. The antiproliferative activity of 2-methoxyestradiol analogs against human cancer cells was investigated. 2-methoxy-3-benzyloxy-17β-chloroacetamide-1,3,5(10)-triene (5e) and 2-methoxy-3-hydroxy-17β-butyramide-1,3,5(10)-triene (6c) had comparable or better antitumor activity than 2-methoxyestradiol. The elimination half-life of 6c (t1/2β = 240.93 min) is ten times longer than 2-ME and the area under the curve was seven times (AUC0-tmin = 2068.20 ± 315.74 μg mL?1 min) higher than 2-ME, respectively. Whereas 5e had similar pharmacokinetic behavior with 2-ME (t1/2β = 22.28 min) with a t1/2β of 29.5 min. 6c had higher blood concentration, longer actuation duration and better suppression rate against S180 mouse ascites tumor than 2-methoxyestradiol.
Synthesis, antitubulin, and antiproliferative SAR of analogues of 2-methoxyestradiol-3,17- O, O -bis-sulfamate
Jourdan, Fabrice,Leese, Mathew P.,Dohle, Wolfgang,Hamel, Ernest,Ferrandis, Eric,Newman, Simon P.,Purohit, Atul,Reed, Michael J.,Potter, Barry V. L.
supporting information; experimental part, p. 2942 - 2951 (2010/08/05)
The synthesis and antiproliferative activity of analogues of estradiol 3,17-O,O-bis-sulfamates (E2bisMATEs) are discussed. Modifications of the C-17 substituent reveal that an H-bond acceptor is essential for high antiproliferative activity. The local env
