768360-55-0Relevant articles and documents
The synthesis, distribution, and anti-hepatic cancer activity of YSL
Ding, Wenfeng,Zhang, Jiali,Yao, Zhi,Lu, Rong,Wu, Dezhu,Li, Ginfu,Shen, Zilong,Sun, Yingji,Lin, Gang,Wang, Chao,Zhao, Ming,Peng, Shiqi
, p. 4989 - 4994 (2004)
(I) HCl/CH3OH; (II) DCC/HOBt/NMM with corresponding carboxyl component; (III) HCl/CH3CO2C2H5 (6 mol/L); (IV) NaOH/H2O/CH3OH; (V) 3H2 and 10% Pd/C. YSL was prepared stepwise from C terminal to N terminal with the side chain un-protective amino acids, Boc-Leu-OMe, Boc-Ser-OH, and Boc-Tyr-OH, as the starting materials in 39.5% total yield (31.2 g/per batch). With the side chain un-protective Boc-(3,5-dibromo)-Tyr-OH and HClA·Ser-Leu-OMe as the starting materials (3,5-3H-Tyr)-Ser-Leu-OH was obtained in 29% yield. The determination of radioactive quantity in the urine and feces indicated that even after the administration for 130 h only 8.4% (5.35% in urine and 3.05% in feces) of total radioactive quantity from the metabolite of [3,5-3H-Tyr]-Ser-Leu-OH were monitored. The distribution study revealed the relative accumulation level of the individual tissue was arranged in the sequence of spleen > liver > kidney > lung > heart > muscle > brain. Selecting hepatic cancer as the target YSL significantly increased the survival time of H22 tumor cells implanted mice.
