98653-15-7Relevant academic research and scientific papers
Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells
Wu, Wei-Cheng,Liu, Yi-Min,Liao, Yu-Hsuan,Hsu, Kai-Cheng,Lien, Ssu-Ting,Chen, I-Chung,Lai, Mei-Jung,Li, Yu-Hsuan,Pan, Shiow-Lin,Chen, Mei-Chuan,Liou, Jing-Ping
, (2020)
A major cause of failure of therapy in patients with non-small cell lung cancer (NSCLC) is development of acquired drug resistance leading to tumor recurrence and disease progression. In addition to the development of new generations of epidermal growth f
Pyrimidinedione-mediated selective histone deacetylase 6 inhibitors with antitumor activity in colorectal cancer HCT116 cells
Liu, Yi-Min,Lee, Hsueh-Yun,Lai, Mei-Jung,Pan, Shiow-Lin,Huang, Hsiang-Ling,Kuo, Fei-Chiao,Chen, Mei-Chuan,Liou, Jing-Ping
, p. 10226 - 10235 (2015/10/28)
We synthesized a series of pyrimidinedione derivatives and evaluated their activities. The results indicate that compound 6, 4-[5-fluoro-2,6-dioxo-3-(tetrahydro-furan-2-yl)-3,6-dihydro-2H-pyrimidin-1-ylmethyl]-N-hydroxy-benzamide, exhibits potent antiproliferative activity, apoptosis induction with cleavage of caspase and PARP, and enhanced tendency to inhibit HDAC6 (IC50 = 12.4 nM) activity over HDAC1 (IC50 = 1710 nM) and HDAC2 (IC50 = 5500 nM). Compound 6 also inhibits tumor growth and is less toxic than parent 4in vivo. These data provide compelling evidence that compound 6 is a potential antitumor compound with HDAC6 targeted inhibitory activity and may be tested for preclinical investigation for cancer treatment.
(o-and p-Nitrobenzyloxycarbonyl)-5-fluorouracil Derivatives as Potential Conjugated Bioreductive Alkylating Agents
Lin, Tai-Shun,Wang, Lin,Antonini, Ippolito,Cosby, Lucille A.,Shiba, David A.,et al.
, p. 84 - 89 (2007/10/02)
A series of (o-and p-nitrobenzyloxycarbonyl)-5-fluorouracil derivatives were synthesized by reacting o- or p-nitrobenzyl chloroformate with 5-fluorouracil in the presence of triethylamine in DMF or Me2SO.The reductive activation of these agents was hypothesized to generate a reactive methide and 5-fluorouracil, two components that are capable of synergistic interaction through complementary inhibition.Measurement of the surviving fractions of EMT6 tumor cells treated with these agents in culture under conditions of hypoxia and aerobiosis resulted in equal cell kill regardless of the state of oxygenation.One of the synthesized agents, 3-(p-nitrobenzyloxycarbonyl)-5-fluorouracil (4), appeared to be superior to 5-fluorouracil in prolonging the survival time of mice bearing intraperitoneal implants of the P388 leukemia and Sarcoma 180.
