Design and synthesis of novel C14-urea-tetrandrine derivatives with potent anti-cancer activity was written by Lan, Junjie;Huang, Lan;Lou, Huayong;Chen, Chao;Liu, Tangjingjun;Hu, Shengcao;Yao, Yao;Song, Junrong;Luo, Jun;Liu, Yazhou;Xia, Bin;Xia, Lei;Zeng, Xueyi;Ben-David, Yaacov;Pan, Weidong. And the article was included in European Journal of Medicinal Chemistry in 2018.HPLC of Formula: 2253-73-8 The following contents are mentioned in the article:
Tetrandrine is a dibenzyltetrahydroisoquinoline alkaloid, isolated from traditional Chinese medicinal plant Stephania tetrandra, with antitumor activity. Our previous study identified several derivatives of tetrandrine showing better activities than parental compound against human hepatocellular carcinoma cells. To increase diversity and cytotoxic activities of the original compound, a series of novel 14-urea-tetrandrine derivatives were synthesized through structural modification of tetrandrine. These derivatives demonstrated a moderate to strong anti-proliferative activities against human cell lines HEL and K562 (Leukemia), prostate (PC3), breast (MDA-MB-231) and melanoma (WM9). Compound I showed strongest cytotoxic effect against PC3 cells with IC50 value of 0.64 μM, which was 12-fold, 31-fold and 26-fold lower than the parental tetrandrine, 5-fluorouracil and cisplatin, resp. Preliminary structure-activity relationship study indicated that urea substitution was the key pharmacophore for the enhancement of their antitumor activities. Induction of apoptosis by I was associated with the activation of pro-apoptotic protein BAX and inhibition of antiapoptosis proteins survivin as well as Bcl-2. Moreover, activation of caspases led to increase cleavage of PARP, which further accelerates apoptotic cell death. These results reveal that the compound I may be used as a potential anticancer drug candidate. This study involved multiple reactions and reactants, such as Isopropylisothiocyanate (cas: 2253-73-8HPLC of Formula: 2253-73-8).
Isopropylisothiocyanate (cas: 2253-73-8) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.HPLC of Formula: 2253-73-8
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics