Synthesis of Icaritin and β-anhydroicaritin Mannich Base Derivatives and Their Cytotoxic Activities on Three Human Cancer Cell Lines

Abstract

Our finding most of icaritin and β-anhydroicaritin Mannich base derivatives possessing moderate to potent cytotoxicity against these three cancer cells (Hela, HCC1954 and SK-OV-3). Compound 15 and 19 showed selective cytotoxicity against HCC1954 cells and Hela cells respectively, they are potential and selective anticancer agent and worthy of further development.

Novel Aminomethyl Derivatives of 4‐Methyl‐2‐prenylphenol: Synthesis and Antioxidant Properties

“…calc. for C 17 (14 (11)); 1.75 (s, 3 H, Me(10)); 2.22 (s, 3 H, ArMe); 2.67 (t, 2 H, J = 7.0, NCH 2 (CH 2 ) 6 Me); 3.32 (d, 2 H, J = 7.2, CH 2 (7)); 3.93 (s, 2 H, ArCH 2 N); 5.35 (br. t, 1 H, J = 6.8, HÀ C(8)); 6.66 (s, 1 H, HÀ C(5)); 6.85 (s, 1 H, HÀ C(3)).…”

“…had a greater cytotoxicity against human cancer cells in a several cases. [14] For Mannich bases derived from prenylated xanthones αand γ-mangostins isolated from Garcinia × mangostana L., an increase in antioxidant (AO) and membrane-protective (MP) properties and a significant decrease in hemolytic activity was shown in most cases. [15] [16] The aim of this work was to synthesize new aminomethyl derivatives containing an ortho-prenylphenol moiety, and to assess the compounds obtained as inhibitors of oxidative processes in vitro.…”

Synthesis and antiproliferative activities of polymethoxyflavones aminoalkyl and amino acid derivatives

“…As part of our screening program dedicated to the search for derivatives of natural flavonoids with anticancer properties [12][13][14][15], we herein synthesized two series of PMFs derivatives by attaching aminoakyl or amino acid moiety through a linking spacer to the free hydroxyl groups at the C-5 position. Furthermore, their antiproliferative activities in vitro against four different human cancer cell lines including Aspc-1 (human pancreatic cancer), SUN-5 (human gastric cancer), HepG-2 (human hepatocellular carcinoma) and HCT-116 (human colon cancer) were evaluated by CCK-8 (cell counting kit-8) assay using Staurosporine as the positive control drug.…”

Synthesis and Biological Evaluation of Novel 5-Oxo-1-Phenylpyrrolidine-3-Carboxylic Acid Analogs

“…Mannich bases received enormous appreciation for their immense realm of applications and many studies have focussed on structural modifications of the Mannich bases and on the vast variety of their biological activities [9,10]. A number of synthetic modifications, such as heterocyclic infused [11,12], thiophene based [13], aurone based mannich bases [14], lawsone based mannich bases [15], berberine based mannich bases [16],or other substitutions [17][18][19][20], have also been reported to affect the biological activities including anticancer activities [21,22] of these bases.…”