80986-13-6

Upstream product

• 2999-18-0 1-(2',4',6'-trihydroxyphenyl)pentan-1-one 
• 77-78-1 dimethyl sulfate 
• 109-72-8 n-butyllithium 
• 3187-19-7 2,4-dimethoxysalicylic acid 
• 80-48-8 methyl p-toluene sulfonate 
• 2082-59-9 pentanoic anhydride 
• 108-73-6 3,5-dihydroxyphenol 

Downstream Products

• 80986-10-3 5,7-dimethoxy-8-pentyl-4-phenylcoumarin 
• 531502-72-4 5,7-dimethoxy-2-(3',4',5'-trimethoxyphenyl)-8-pentyl-4H-chromen-4-one 
• 531502-63-3 1-(2-hydroxy-4,6-dimethoxy-3-pentyl-phenyl)-ethanone 
• 80986-12-5 2-n-pentyl-3,5-dimethoxyphenol 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance

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.

Rational design of inhibitors of VirA-VirG two-component signal transduction

VirA-VirG two-component system regulates the vir (virulence) operon in response to specific host factors (xenognosins) in the plant pathogen Agrobacterium tumefaciens. Using whole cell assays, stable inhibitors inspired by the labile natural benzoxazinone inhibitor HDMBOA are developed. It is found that aromatic aldehydes represent a minimal structural unit for activity. In particular, 3-hydroxy-4,6-dimethoxy-3H-isobenzofuran-1-one (HDI) was found to have the highest activity, making it the most potent developed inhibitor of virulence gene expression in Agrobacterium.

Synthesis of novel flavonoid derivatives as potential HIV-integrase inhibitors

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.