Design, synthesis, and biological evaluation of new 12-substituted-14-deoxy-andrographolide derivatives as apoptosis inducers

Synthetic Modifications of Andrographolide Targeting New Potential Anticancer Drug Candidates: A Comprehensive Overview

“…Dysfunctional angiogenesis has been associated with the development of several diseases, including cancers [ 31 ]. It should be noted that inflammation and angiogenesis are closely linked, making andrographolide a prime raw material for the development of drug candidates [ 31 , 32 ]. Indeed, andrographolide inhibits vascular endothelial growth factor (VEGF)-mediated tumor angiogenesis by binding to vascular endothelial growth factor receptor 2 (VEGFR2), thus exhibiting an antitumor effect [ 33 ].…”

“…To assess the potential for apoptosis induction in the HCT-116 cell line, Kandanur et al synthesized an array of compounds bearing diverse substituents at the C12 position of 3,19-di- O -acetyl-C-12-substituted-14-deoxy-andrographolide [ 32 ]. The most active derivative had a (2-methylthio)phenylamino group at the C12 position ( Figure 14 ).…”

(3,19)‐4‐Bromobenzylidene‐isoandrographolide Induces Apoptosis and Causes Loss of Mitochondrial Membrane Potential in MCF‐7 Breast Cancer Cells

“…In our previous studies, various andrographolide derivatives were synthesized by introducing alkyl amines, benzyl amines, phenyl thio, and sulphonamide moiety at C-12 and reported to have superior anticancer activity than the parent compound andrographolide itself. [18][19][20][21] We have also synthesized acetals of andrographolide and its isomers (isoandrographolide and 14deoxy-12-hydroxyandrographolide) using heteroaromatic aldehydes and unsubstituted benzaldehyde and reported their anticancer activity. In this study acetals of isoandrographolide synthesized using unsubstituted benzaldehyde showed improved anticancer activity.…”