26307-85-7Relevant articles and documents
Design, synthesis and biological evaluation of novel L-isoserine tripeptide derivatives as aminopeptidase N inhibitors
Pan, Huili,Yang, Kanghui,Zhang, Jian,Xu, Yingying,Jiang, Yuqi,Yuan, Yumei,Zhang, Xiaopan,Xu, Wenfang
, p. 717 - 726 (2013/07/26)
Aminopeptidase N (APN/CD13) is one of the essential proteins for tumour invasion, angiogenesis and metastasis as it is over-expressed on the surface of different tumour cells. Based on our previous work that L-isoserine dipeptide derivatives were potent APN inhibitors, we designed and synthesized L-isoserine tripeptide derivatives as APN inhibitors. Among these compounds, one compound 16l (IC50=2.51±0.2 M) showed similar inhibitory effect compared with control compound Bestatin (IC50=6.25±0.4 M) and it could be used as novel lead compound for the APN inhibitors development as anticancer agents in the future.
Cyclic dipeptides exhibit potency for scavenging radicals
Furukawa, Tadashi,Akutagawa, Takashi,Funatani, Hitomi,Uchida, Toshikazu,Hotta, Yoshihiro,Niwa, Masatake,Takaya, Yoshiaki
, p. 2002 - 2009 (2012/05/04)
Twenty kinds of cyclic dipeptides containing l-leucine were synthesized, and their antioxidant activity against .OH and O2·- was investigated. Compounds possessing polar amino acid residues, such as Asp, Cys, Glu, Lys, Pro, Ser, and Trp, exhibited higher antioxidant activity against .OH than vitamin E. However, only cyclo(l-Cys-l-Leu) scavenged O2·-.
Synthesis of [12]aneN3-dipeptide conjugates as metal-free DNA nucleases
Li, Zhi-Fen,Chen, Hua-Long,Zhang, Li-Jun,Lu, Zhong-Lin
supporting information; experimental part, p. 2303 - 2307 (2012/05/04)
In this Letter, a series of macrocyclic polyamine [12]aneN 3-dipeptide conjugates as a new type of metal-free nucleases were synthesized and fully characterized with 1H NMR, 13C NMR, IR, and HR-MS. Results indicate that th
Syntheses of [12]aneN3-oligopeptide conjugates as effective DNA condensation agents
Li, Zhi-Fen,Guo, Zhi-Fo,Yan, Hao,Lu, Zhong-Lin,Wu, Da-Yong
supporting information; experimental part, p. 2897 - 2904 (2012/07/14)
With the aim to develop effective and low toxicity DNA condensation agents, a series of oligopeptide derived macrocyclic polyamine [12]aneN3 conjugates 7a-h·3HCl have been designed and synthesized through multi-step amidation reactions. Structu
Efficient synthesis of 2,5-diketopiperazines using microwave assisted heating
Tullberg, Marcus,Gr?tli, Morten,Luthman, Kristina
, p. 7484 - 7491 (2007/10/03)
In this study a general, efficient and environmentally benign solution phase synthesis of 2,5-diketopiperazines (DKPs) using microwave assisted heating in water is described. A series of 11 structurally different DKPs have been synthesized from dipeptide methyl esters. A range of common laboratory solvents have been tested as well as different reaction times and temperatures. Both classic thermal and microwave assisted heating have been investigated. Microwave assisted heating for 10 min using water as solvent proved, by far, to be the most efficient method of cyclization giving moderate to excellent yields (63-97%) of DKPs. In contrast to other published procedures, this method seems independent of the amino acid sequence.
COMPOUNDS USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES
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Page 18, (2010/02/08)
There are provided according to the invention, novel compounds of formula (I)wherein R, R, R, R, Rand Rare as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.