297740-86-4Relevant academic research and scientific papers
Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas
Daniele, Simona,La Pietra, Valeria,Barresi, Elisabetta,Di Maro, Salvatore,Da Pozzo, Eleonora,Robello, Marco,La Motta, Concettina,Cosconati, Sandro,Taliani, Sabrina,Marinelli, Luciana,Novellino, Ettore,Martini, Claudia,Da Settimo, Federico
, p. 4526 - 4538 (2016)
In glioblastoma multiforme (GBM), translocator protein (TSPO) and murine double minute (MDM)2/p53 complex represent two druggable targets. We recently reported the first dual binder 3 possessing a higher anticancer effect in GBM cells than the standards P
Marine natural occurring 2,5-diketopiperazines: Isolation, synthesis and optical properties
Laville, Rmi,Nguyen, Thanh Binh,Moriou, Cline,Petek, Sylvain,Debitus, Ccile,Al-Mourabit, Ali
, p. 1351 - 1366 (2015/03/04)
Seven 2,5-diketopiperazines (DKPs) were isolated from the Fijian marine sponge Acanthella cavernosa. NMR and circular dichroism (CD) comparison with synthetic L-L DKPs allowed us to determine unambiguously the L-L absolute configuration of the natural DKPs. This work initiated the setting up of an optical properties database of natural DKPs, including specific rotation and CD.
Solvent-free peptide synthesis assisted by microwave irradiation: Environmentally benign synthesis of bioactive peptides
Mahindra, Amit,Patel, Neha,Bagra, Nitin,Jain, Rahul
, p. 3065 - 3069 (2014/01/06)
An efficient and facile, solvent-free peptide synthesis assisted by microwave irradiation, using DIC/HONB as the coupling reagent combination is reported. Key features of this original protocol are solvent-free synthesis, very short reaction time and scal
Microwave-assisted solution phase peptide synthesis in neat water
Mahindra, Amit,Nooney, Karthik,Uraon, Shrikant,Sharma, Krishna K.,Jain, Rahul
, p. 16810 - 16816 (2013/09/23)
An environmentally benign protocol for solution phase peptide synthesis has been developed in neat water using TBTU/HOBt/DIEA as a coupling combination under microwave irradiation. Key features of this procedure are the replacement of commonly used toxic organic solvents like DMF and NMP, the use of lower amounts of reactants, compatibility with both N-α-Boc- and N-α-Fmoc-protected amino acids and all commonly used side-chain protective groups, short reaction time, and racemization-free synthesis in high yield and purity. The Royal Society of Chemistry 2013.
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.
Synthesis, cytotoxic and antimicrobial screening of a proline-rich cyclopolypeptide
Dahiya, Rajiv,Kumar, Akhilesh,Gupta, Rajul
body text, p. 214 - 217 (2009/10/02)
Present study describes the first total synthesis of a cyclic heptapeptide, stylisin 1 (8) via coupling of tetrapeptide Boc-L-tyrosinyl-L-prolyl-L-leucyl- L-proline-OH and tripeptide L-phenylalanyl-L-isoleucyl-L-proline- OMe followed by cyclization of lin
Cyclopeptide alkaloids from Paliurus ramossisimus
Lin,Chen,You,Chen Liu,Lee
, p. 1338 - 1343 (2007/10/03)
Seven zizyphine A-type cyclopeptide alkaloids were isolated from the roots of Paliurus ramossisimus by the combination of centrifugal partition chromatography and conventional separation methods. The novel structures of paliurines A-F (1-6) were characterized and established on the basis of MS and elaborate NMR spectral analyses. Terminal dipeptide stereochemistry was confirmed by correlation with the synthetic dipeptides via comparison of their 13C NMR data.
