The curcumin molecule is unique in its physiological effects in having a greater number of molecular targets than any other molecule so far reported. Extensive structure activity relationship sar studies have been carried out on the curcumin molecule and its synthetic analogues.
Figure 1 From Structure Activity Relationships Of The Antitumor C5
Structure Activity Relationships Of Curcumin Analogs Download
Structure Activity Relationships Of Curcumin Analogs Download
Natural analogues and structure activity relationship cancers have been found to be the leading causes of death worldwide with 82 million.
Curcumin structure activity relationship. Screen of curcumin analogs on upregulation of nep by activity assay. In this activity assay we measured the fluorescence increase caused by cleavage of a quenched fluorogenic peptide qf ab 1 7c which can be cleaved by nep and ide but not by other ab degrading enzymes fig. Curcumin a dietary compound from turmeric has beneficial effects on inflammatory diseases such as inflammatory bowel disease.
Intrigued by the potent antitumor activity of c5 curcumin 2 related 15 bisaryl 14 pentadiene 3 ones bisarylmethylideneacetones termed c5 curcuminoids we previously conducted a structureactivity relationship study of c5 curcuminoids and showed that highly active go y030 15 bis35 bismethoxymethoxyphenyl 14 pentadiene 3 one 4 is the most promising antitumor compound. Elimination of the 4 oh groups compound 1 or incorporation of an additional och 3 group compound 4 onto curcumin resulted in a slight decrease in anti proliferative activities. Crossref medline cas google scholar 116 qin hl leng j zhang cp et al.
Since nep is an ectoenzyme. Structureactivity relationship of curcumin analogs as multifuntional agents. Structureactivity relationships of amyloid betaaggregation inhibitors based on curcumin.
Since then curcumin has been noted in more than 4000 reports on the wide spectrum of biological activities from antioxidant to anti inflammatory to anticancer. Influence of linker length and flexibility ashley a. Most previous studies have focused on the structureactivity relationship of the thiol reactive ab unsaturated carbonyl groups of curcumin so little is known about the roles of methoxy groups in biological activities of curcumin.
Our first structureactivity relationship study was to investigate the substitution pattern of the 3 och 3 and 4 oh groups on the aromatic ring in curcumin. Curcumin is a natural polyphenol product derived from the rhizome of the curcuma longa. Reinke department of pathology and the life sciences institute university of michigan ann arbor michigan 481092216 usa.
Structure activity relationship in modern medicine the first curcumin study on human diseases was reported in 1937 by oppenheimer. Request pdf on researchgate anticancer curcumin. In vivo and in vitro studies have uncovered many important bioactivities of curcumin such as antioxidant activity inducing cell apoptosis inhibiting cell proliferation anti cell adhesion and motility anti angiogenesis and anti microbe properties.
Synthesis of a b unsaturated carbonyl based compounds oxime and oxime ether analogs as potential anticancer agents for overcoming cancer multidrug resistance by modulation of efflux pumps in tumor cells.
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