Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors was written by Du, Lifei;Wang, Xiaoyu;Cui, Guonan;Xu, Bailing. And the article was included in Bioorganic & Medicinal Chemistry in 2021.Recommanded Product: 4-Methylpiperidin-4-ol hydrochloride This article mentions the following:
Pin1 is a peptidyl prolyl cis-trans isomerase (PPIase) and inhibiting Pin1 is a potential way for discovering anti-tumor agents. With an aim to find potent Pin1 inhibitors with a novel scaffold, a series of thiazole derivatives with an alicyclic heterocycles on the 2-position were designed, synthesized and tested against human Pin1. Compound 9p bearing a 2-oxa-6-azaspiro [3,3] heptane moiety on the thiazole scaffold was identified as the most potent Pin1 inhibitor of this series with an IC50 value of 0.95μM. The structure-activity relationship (SAR) and mol. modeling study indicated that introducing an alicyclic ring with an H-bond acceptor would be a viable way to improve the binding affinity. In the experiment, the researchers used many compounds, for example, 4-Methylpiperidin-4-ol hydrochloride (cas: 586375-35-1Recommanded Product: 4-Methylpiperidin-4-ol hydrochloride).
4-Methylpiperidin-4-ol hydrochloride (cas: 586375-35-1) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Recommanded Product: 4-Methylpiperidin-4-ol hydrochloride
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem