Reference of tert-Butyl (5-aminopentyl)carbamateIn 2019 ,《Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the “”Selectivity Pocket””, Substrate-Binding Site, and NAD+-Binding Site》 was published in Journal of Medicinal Chemistry. The article was written by Mellini, Paolo; Itoh, Yukihiro; Elboray, Elghareeb E.; Tsumoto, Hiroki; Li, Ying; Suzuki, Miki; Takahashi, Yukari; Tojo, Toshifumi; Kurohara, Takashi; Miyake, Yuka; Miura, Yuri; Kitao, Yuki; Kotoku, Masayuki; Iida, Tetsuya; Suzuki, Takayoshi. The article contains the following contents:
The NAD+-dependent deacetylase SIRT2 represents an attractive target for drug development. Here, we designed and synthesized drug-like SIRT2-selective inhibitors based on an anal. of the putative binding modes of recently reported SIRT2-selective inhibitors and evaluated their SIRT2-inhibitory activity. This led us to develop a more drug-like diketopiperazine structure as a “”hydrogen bond (H-bond) hunter”” to target the substrate-binding site of SIRT2. Thioamide 53, a conjugate of diketopiperazine and 2-anilinobenzamide which is expected to occupy the “”selectivity pocket”” of SIRT2, exhibited potent SIRT2-selective inhibition. Inhibition of SIRT2 by 53 was mediated by the formation of a 53-ADP-ribose conjugate, suggesting that 53 is a mechanism-based inhibitor targeting the “”selectivity pocket””, substrate-binding site, and NAD+-binding site. Furthermore, 53 showed potent antiproliferative activity toward breast cancer cells and promoted neurite outgrowth of Neuro-2a cells. These findings should pave the way for the discovery of novel therapeutic agents for cancer and neurol. disorders. After reading the article, we found that the author used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Reference of tert-Butyl (5-aminopentyl)carbamate)
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Reference of tert-Butyl (5-aminopentyl)carbamate
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