Synthesis and FKBP binding of small molecule mimics of the tricarbonyl region of FK506 was written by Wang, Gary T.;Lane, Ben;Fesik, Stephen W.;Petros, Andrew;Luly, Jay;Krafft, Grant A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1994.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:
Small acyclic model compounds were synthesized to examine the importance of the C(9) carbonyl group of FK506 for FKBP binding. 4-(4′-Methoxyphenyl)-1-Bu (3”,4”,5”-trimethoxyphenylglyoxyl)pipecolate, containing the N-(glyoxyl)pipecolate motif of FK506, was found to bind to FKBP with IC50 of 16 μM. Replacement of the carbonyl group at the position corresponding to C(9) of FK506 with small nonpolar groups (hydrogen, methylene or Me group) significantly reduced the binding affinity. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: 86069-86-5).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 86069-86-5
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem