102971-73-3Relevant articles and documents
The mimics of Nε-acyl-lysine derived from cysteine as sirtuin inhibitors
Wang, Chun,Wang, Fang,Chen, Xiaoxue,Zou, Yefang,Zhu, Hong,Zhao, Qingjie,Shen, Jingshan,Li, Yan,Li, Yongjun,He, Bin
, p. 2375 - 2378 (2018)
Sirtuin inhibitors as physiological research tools and therapeutic potentials have caught many attentions in last decades. The mimics of acyl lysine have been approved to be a very efficient strategy for development of mechanism-based sirtuin inhibitors. In current study, a novel scaffold of L-S-(3-carboxamidopropyl) cysteine (L-CAPC) has been exploited for design and synthesis of sirtuin inhibitors. As a result, the mimics of Nε-acyl-lysine derived from cysteine including small molecules (5a–m) and peptides (9a–m) have been synthesized. Among these, the peptides 9g and 9h were found to be the most inhibitory potency and selectivity against SIRT2.
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine
Glenn, Matthew P.,Kahnberg, Pia,Boyle, Glen M.,Hansford, Karl A.,Hans, Dhiraj,Martyn, Adam C.,Parsons, Peter G.,Fairlie, David P.
, p. 2984 - 2994 (2004)
Selective destruction of malignant tumor cells without damaging normal cells is an important goal for cancer chemotherapy in the 21st century. Differentiating agents that transform cancer cells to either a nonproliferating or normal phenotype could potent
1-deamino-1(15)-carba and -dicarba analogues of endothelin-1
Hlavacek, Jan,Marcova, Renata,Budesinsky, Milos,Slaninova, Jirina
, p. 407 - 424 (2007/10/03)
Sulfanyl-methylene and ethylene bridges were inserted into the molecule of endothelin-1 (ET-1) as other possible isosteric replacements of its outer disulfide linkage. The [1-deamino-1-carba]ET-1, [1-deamino-15-carba]ET-1 and [1-deamino-1,15-dicarba]ET-1 were synthesized either by a fragment condensation of protected cyclic pentadecapeptides with carboxy-terminal hexapeptides of the endothelin-1 sequence or by step-wise coupling on polymer support of the entire henicosapeptide sequences from carboxy-terminus. The analogues were devoid of uterotonic activity in comparison with the parent ET-1.