2095677-20-4Relevant academic research and scientific papers
Discovery of Novel 5-(Piperazine-1-carbonyl)pyridin-2(1H)-one Derivatives as Orally eIF4A3-Selective Inhibitors
Mizojiri, Ryo,Nakata, Daisuke,Satoh, Yoshihiko,Morishita, Daisuke,Shibata, Sachio,Iwatani-Yoshihara, Misa,Kosugi, Yohei,Kosaka, Mai,Takeda, Junpei,Sasaki, Shigekazu,Takami, Kazuaki,Fukuda, Koichiro,Kamaura, Masahiro,Sasaki, Shinobu,Arai, Ryosuke,Cary, Douglas R.,Imaeda, Yasuhiro
, p. 1077 - 1082 (2017)
Starting from our previous eIF4A3-selective inhibitor 1a, a novel series of (piperazine-1-carbonyl)pyridin-2(1H)-one derivatives was designed, synthesized, and evaluated for identification of orally bioavailable probe molecules. Compounds 1o and 1q showed improved physicochemical and ADMET profiles, while maintaining potent and subtype-selective eIF4A3 inhibitory potency. In accord with their promising PK profiles and results from initial in vivo PD studies, compounds 1o and 1q showed antitumor efficacy with T/C values of 54% and 29%, respectively, without severe body weight loss. Thus, our novel series of compounds represents promising probe molecules for the in vivo pharmacological study of selective eIF4A3 inhibition.
Heterocyclic compounds
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Paragraph 0193, (2018/04/20)
[A] compounds useful in treating or preventing cancer containing a drug. The present invention is [a], formula (I):[In the formula, each symbol is as defined herein. ]The compound or its salt represented by the related. [Drawing] no
