Synthesis and structure-activity relationships of novel, potent, orally active hypoxia-inducible factor-1 inhibitors was written by Nagao, Satoshi;Yamane, Yoshinobu;Funasaka, Setsuo;Tanaka, Keigo;Miyazaki, Kazuki;Kotake, Yoshihiko;Kamata, Jun-ichi;Watanabe-Miyano, Saori;Toyama, Osamu;Ozawa, Yoichi;Mizui, Yoshiharu;Okamoto, Kiyoshi;Ito, Daisuke. And the article was included in Bioorganic & Medicinal Chemistry in 2014.SDS of cas: 147081-29-6 This article mentions the following:
Hypoxia-inducible factor-1 (HIF-1) is the chief transcription factor regulating hypoxia-driven gene expression. HIF-1 overexpression is associated with poor prognosis in several cancers and therefore represents an attractive target for novel antitumor agents. The authors explored small mol. inhibitors of the HIF-1 pathway. Using high-throughput-screening, the authors identified a benzanilide compound (IC50 = 560 nM) as a seed. Subsequent extensive derivatization led to the discovery of compounds I and II d, with anti-HIF-1 activities in vitro (IC50 = 21 and 0.47 nM, resp.), and in vivo. Addnl., I (12.5-100 mg/kg) also displayed in vivo antitumor efficacy, without influencing body weight In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6SDS of cas: 147081-29-6).
(S)-tert-Butyl 3-methylpiperazine-1-carboxylate (cas: 147081-29-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.SDS of cas: 147081-29-6
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics