Ma, Junjie; Ni, Xin; Gao, Yali; Huang, Kun; Wang, Yu; Liu, Jiaan; Gong, Guowei published the artcile< Semicarbazone derivatives bearing phenyl moiety: synthesis, anticancer activity, cell cycle, apoptosis-inducing and metabolic stability study>, HPLC of Formula: 611-19-8, the main research area is semicarbazone phenyl preparation antitumor activity; anticancer activity; apoptosis; metabolic stability; semicarbazone; sub-G1.
A series of semicarbazone derivatives bearing Ph moiety I [R = Me, Et; R1 = H, benzyloxidanyl, 2-(2H-1,3-benzodioxol-5-ylmethyl)-(1,3-thiazol-4-yl)-methyloxy, [(4-chlorophenyl)methyl]oxidanyl, etc.; R2 = t-Bu, H, prop-2-en-1-yl; R3 = H, t-Bu] was synthesized and evaluated for the vitro anticancer activities in four human cancer cell lines (human colon cancer (HT29), human neuroblastoma (SK-N-SH), human breast cancer (MDA-MB-231), and human gastric cancer (MKN45)). Biol. evaluation led to the identification of I [(I) R = Me, R1 H, R2 = R3 = t-Bu; (II) R = Et, R1 H, R2 = R3 = t-Bu], which showed excellent anticancer activities against tested cancer cell lines with IC50 values ranging from 0.32 to 1.57 μM, resp., while exhibiting weak cytotoxicity on the normal cells (human umbilical vein endothelial cell (HUVEC)). Flow cytometric assay for cell cycle and apoptosis revealed that (I) and (II) caused an arrest in the Sub-G1 cell cycle and inhibited proliferation of cancer cells by inducing apoptosis in a dose-dependent manner. Further enzymic assay suggested that (I) and (II) could significantly activated procaspase-3 to caspase-3. Metabolic stability study indicated that (I) and (II) showed moderate stability in vitro in human and rat liver microsomes. In view of promising pharmacol. activities of (I) and (II), which had emerged as the valuable lead for further development in the treatment for cancer.
Chemical & Pharmaceutical Bulletin published new progress about Antitumor agents. 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, HPLC of Formula: 611-19-8.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics