Reference of 2-(Piperidin-4-yl)ethanolIn 2020 ,《Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent》 was published in Journal of Medicinal Chemistry. The article was written by Kurasawa, Osamu; Miyazaki, Tohru; Homma, Misaki; Oguro, Yuya; Imada, Takashi; Uchiyama, Noriko; Iwai, Kenichi; Yamamoto, Yukiko; Ohori, Momoko; Hara, Hideto; Sugimoto, Hiroshi; Iwata, Kentaro; Skene, Robert; Hoffman, Isaac; Ohashi, Akihiro; Nomura, Toshiyuki; Cho, Nobuo. The article contains the following contents:
In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported thieno[3,2-d]pyrimidinone analog I showing time-dependent Cdc7 kinase inhibition and slow dissociation kinetics. These medicinal chem. efforts led to the identification of compound 3d, which exhibited potent cellular activity, excellent kinase selectivity, and antitumor efficacy in a COLO205 xenograft mouse model. However, the issue of formaldehyde adduct formation emerged during a detailed study of 3d, which was deemed an obstacle to further development. A structure-based approach to circumvent the adduct formation culminated in the discovery of compound 11b (TAK-931) possessing a quinuclidine moiety as a preclin. candidate. In this paper, the design, synthesis, and biol. evaluation of this series of compounds will be presented. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Reference of 2-(Piperidin-4-yl)ethanol)
2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKReference of 2-(Piperidin-4-yl)ethanol
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem