80986-12-5Relevant academic research and scientific papers
Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance
Yin, Huanhuan,Dong, Jingjing,Cai, Yingchun,Shi, Ximeng,Wang, Hao,Liu, Guixia,Tang, Yun,Liu, Jianwen,Ma, Lei
, p. 350 - 366 (2019/07/19)
Overexpression of P-glycoprotein (P-gp) is one of the major causes for multidrug resistance (MDR), which has become a major obstacle in cancer therapy. One hopeful approach to reverse the MDR is to develop inhibitors of P-gp in expression and/or function. Here, we designed and synthesized a series of chalcone derivatives as P-gp inhibitors and evaluated their potential reversal activities against MDR. Among them, the most active compound MY3 had little intrinsic cytotoxicity and showed the highest activity (RF = 50.19) in reversing DOX resistance in MCF-7/DOX cells. Further studies demonstrated that MY3 could increase intracellular accumulation of DOX and inhibit expression of P-gp at mRNA and protein levels. More importantly, MY3 significantly enhanced the efficacy of DOX against the tumor xenografts bearing MCF-7/DOX cells with the precondition of unchanged body weight. Therefore, MY3 might represent a promising lead to develop MDR reversal agents for cancer chemotherapy.
Regioselective synthesis and estrogenicity of (±)-8-alkyl-5,7- dihydroxy-4-(4-hydroxyphenyl)-3,4-dihydrocoumarins
Roelens, Frederik,Huvaere, Kevin,Dhooge, Willem,Van Cleemput, Marjan,Comhaire, Frank,De Keukeleire, Denis
, p. 1042 - 1051 (2007/10/03)
Nine new (±)-8-alkyl-5,7-dihydroxy-4-(4-hydroxyphenyl)-3,4- dihydrocoumarins have been synthesized from 2,4,6-trimethoxybenzaldehyde via a short, efficient, and regioselective pathway, together with the unsubstituted analogue (±)-5,7-dihydroxy-4-(4-hydroxyphenyl)-3,4-dihydrocoumarin. The compounds were tested for estrogenic activity using a yeast-based estrogen screen. Weak estrogenicity was determined for seven members of the series.
Synthesis of novel flavonoid derivatives as potential HIV-integrase inhibitors
Mateeva, Nelly N.,Kode, Rao N.,Redda, Kinfe K.
, p. 1251 - 1258 (2007/10/03)
Eighteen novel flavonoid derivatives - substituted chalcones and flavones were synthesized and characterized by using NMR, IR, UV/Vis spectroscopy and elemental analysis. The target compounds were achieved by using a sequence of simple and effective reactions starting from phloroglucinol. The initial hydroxyl groups were protected by methylation and in the final flavones the 5-OH group was selectively demethylated by means of AlBr3. 5-methoxy flavones exhibit a strong fluorescence, which was quenched after the removal of the methyl group.
Synthesis of Alkyl Substituted 4-Phenylcoumarins
Ahluwalia, V. K.,Mukherjee, Irani,Rani, Nimmi
, p. 918 (2007/10/02)
4-Phenylcoumarins substituted in position-8 by alkyl groups (ethyl, n-propyl and n-pentyl) have been synthesised in good yields by the condensation of 2-ethyl-3,5-dimethoxyphenol, 3,5-dimethoxy-2-propylphenol and 3,5-dimethoxy-2-pentylphenol, respectively
