18658-65-6Relevant articles and documents
Effect of the 4′-substituted phenylalanine moiety of sansalvamide A peptide on antitumor activity
Liu, Shouxin,Yang, Yihua,Zhao, Cuiran,Huang, Jing,Han, Chunyu,Han, Jianrong
, p. 463 - 467 (2014/04/17)
Eight sansalvamide A peptide analogues with 4′-fluoride, 4′-chloride, 4′-bromide, 4′-iodide, and 4′- methoxyphenylalanine moieties were synthesized. The effect of these para-substitutions of sansalvamide A peptide on their cytotoxicity was evaluated using HCT-116, MDA-MB-231, HT-29, HCT-15, K562, HeLa, and A549 cell lines. The 4′-methoxyphenylalanine analog of sansalvamide A peptide was found to be a promising antitumor agent.
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
experimental part, 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, antimicrobial and anthelmintic activity of 2-amino-4-phenylthiazole derivatives of amino acids and peptides
Himaja,Raju, V. Kishore,Ranjitha
experimental part, p. 2909 - 2913 (2010/11/05)
A novel series of 2-amino-4-phenylthiazole derivatives of amino acids and peptides were synthesized by solution phase technique. The synthesized compounds were characterized by FTIR, 1H NMR and mass spectral analysis and evaluated for their antibacterial, antifungal and anthelmintic activities. The compounds exhibited significant antifungal and anthelmintic activities as compared to standard drugs fluconazole and mebendazole, respectively.
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 17-18, (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.
Studies of selective Boc removal in the presence of silyl ethers
Cavelier, Florine,Enjalbal, Christine
, p. 5131 - 5134 (2007/10/03)
The selective removal of N-Boc protection can be obtained in the presence of either TBDMS or TBDPS ethers. On the basis of promising results from the literature, we first tried sonication, that failed, whereas the exclusive cleavage of the Boc group was successfully achieved by a saturated solution of HCl in ethyl acetate.