1354972-75-0Relevant academic research and scientific papers
Isothiouronium modification empowers pyrimidine-substituted curcumin analogs potent cytotoxicity and Golgi localization
Tong, Sheng,Zhang, Meng,Wang, Shixi,Yin, Ruijuan,Yu, Rilei,Wan, Shengbiao,Jiang, Tao,Zhang, Lijuan
, p. 849 - 857 (2016)
Most of protein post-translational modifications occur in the Golgi and many human diseases are associated with abnormal Golgi function or improper post translational modifications of proteins in the Golgi. In this study, we designed and synthesized 4?×?6
Exploring pyrimidine-substituted curcumin analogues: Design, synthesis and effects on EGFR signaling
Qiu, Peiju,Xu, Lingling,Gao, Lei,Zhang, Meng,Wang, Shixi,Tong, Sheng,Sun, Yue,Zhang, Lijuan,Jiang, Tao
, p. 5012 - 5020 (2013/09/02)
Epidermal growth factor receptor (EGFR) is an effective molecular target of anti-cancer therapies. Curcumin inhibits cancer cell growth in vitro by suppressing gene expression of EGFR and reduces tumor growth in various animal models. To overcome instable and insoluble properties of curcumin as therapeutics, we designed and synthesized six novel pyrimidine-substituted curcumin analogues with or without a hydroxyl group originally present in curcumin. The cell viability tests indicated that IC50 of the analogues containing hydroxyl group were 3 to 8-fold lower than those of the analogues without hydroxyl group in two colon cancer cell lines tested. Western blot analysis indicates the analogues containing hydroxyl group inhibited expression and tyrosine phosphorylation of EGFR. Further protein analyses showed that the analogues had anti-cellular proliferation, pro-apoptosis, and cell cycle arrest properties associated with suppressed EGFR expression. These results indicate that the hydroxyl groups in curcumin and the analogues were critical for observed biological activities.
Synthesis of a novel series of (E, E)-4,6-bis(styryl)-2-O-glucopyranosyl- pyrimidines and their potent multidrug resistance (MDR) reversal activity against cancer cells
Gao, Lei,Liu, Qian,Ren, Sumei,Wan, Shengbiao,Jiang, Tao,Wong, Iris L. K.,Chow, Larry M. C.,Wang, Shixi
, p. 620 - 633 (2013/01/16)
A novel series of methoxy or benzyloxy substituted (E,E)-4,6-bis(styryl)-2- O-glucopyranosyl-pyrimidines as curcuminoid analogs were synthesized in four steps with total yields of 21.5% to 33.9%. A549 and HL60 cells were employed for the anticancer activity testing. The results demonstrated that 5a, 5c, and 5e have some inhibitory activity against the HL-60 cell line. Unfortunately, no compound displayed inhibitory activity against A549 except for 5c. MDR reversal activity results demonstrated that compounds 4a (RF = 12.3) and 4b (RF = 18.5) showed strong reversal activity to the P-gp-mediated LCC6MDR cells compared to verapamil (RF = 3.2) and no cytotoxicity to cancer or normal cell lines even at a high concentrations (100M).
