Design, synthesis, and biological evaluation of angiogenesis inhibitors: aromatic enone and dienone analogues of curcumin

Design, synthesis and biological evaluation of Novel Curcumin Analogs with anticipated anticancer activity

“…That was reachable through natural product compounds which were found to be a good source for both novel and potent bioactive compounds with minimal side effects in vivo [1][2][3][4][5][6][7][8][9][10] .…”

Synthesis of alkylsulfonyl and substituted benzenesulfonyl curcumin mimics as dual antagonist of L-type Ca2+ channel and endothelin A/B2 receptor

“…6 Based on its diverse and interesting biological properties, we previously reported the synthesis of a curcumin mimic library and described the novel biological properties of each member after first report by Bowen and co-workers. 7 For example, the alkyl or aryl amide-linked curcumin mimic library (2) was shown to inhibit angiogenesis 8 and multidrug resistance (MDR). 9,10 Substituted triazolyl curcumin mimics (3 and 4) synthesized through click reaction exhibited strong inhibitory activity against osteoclastogenesis induced by the receptor activator of NF-jB ligand (RANKL).…”

“…Several years ago, we synthesized an alkyl or aryl sulfonyl amide curcumin mimic library (7) and reported that library members exhibit a vasodilatation effect on the depolarization (50 mM K + )-induced basilar arterial contraction ex vivo. 16 Therefore, it seems reasonable to conclude that the sulfonyl amide linked curcumin library (7) has a potential to control vascular tone.…”

“…16 Therefore, it seems reasonable to conclude that the sulfonyl amide linked curcumin library (7) has a potential to control vascular tone. Considering this, we extended our research of the basic vasodilation property of curcumin mimics (7) in order to evaluate the clinical potential for treating vascular related diseases (Fig. 1).…”

Syntheses and Cytotoxic Properties of the Curcumin Analogs 2,6‐Bis(benzylidene)‐4‐phenylcyclohexanones

“…These analogs replaced the diketone moiety of curcumin with a 4-phenylcyclohexanone moiety. Cyclohexanone analogs that lack the 4-phenyl group have recently been reported and they were discovered to have significant anti-angiogenic activity, measured by the inhibition of the growth of SVR endothelial cells in culture [18]. Substituted heterocyclic analogs of curcumin namely various 3,5-bis(benzylidene)-4-piperidones have also been reported and they were found to be active in inhibiting the growth of cancer cells in culture [19,20].…”