title: Synthesis of Novel Imine Stilbene Analogs Exhibiting Potent Anticancer Activity.
abstract: BACKGROUND
  Resveratrol (RV) and its analogues Aza-stilbenes were found effective in exhibiting anticancer activity.
  
  
  OBJECTIVE
  The present study mainly focused on the green synthesis of novel imine stilbene analogues and evaluation of their anticancer activity besides their influence on hypoxia-induced gene expression in cancer cells.
  
  
  METHODS
  Novel imine stilbenes, differing in number and/or position of hydroxyl and methoxy functional groups, have been synthesized using green chemistry mediated condensation reaction between aldehydes and amines in the ethanolic extract of Psoralea corylifolia hairy roots and tested for their anticancer potential.
  
  
  RESULTS
  Ethanol containing 1% hairy root extract facilitated instant reaction and yielded more than 99% product( s). MTT assay on HeLa cells treated with imine stilbene analogues revealed an increase in the inhibition of cell proliferation as compared to RV. Treatment of nontumor HEK293 cells with these compounds disclosed minimal toxicity implying the selective advantage of these compounds for cervical cancer therapy. Scratch assay on HeLa cells displayed inhibition of directional cell motility by these analogues and compound 3e [4-((E)-(4- hydroxyphenylimino)methyl)-2-methoxyphenol] recorded maximum inhibition. In reporter assay, as compared to untreated N-(2-Methoxy-2-oxoacetyl) glycine methyl ester (DMOG) induced cells, hypoxia response element- directed transcriptional activity has been significantly reduced in DMOG induced cells treated with imine stilbene analogues.
  
  
  CONCLUSIONS
  Overall results indicated that four of the five imine stilbene analogues exhibited enhanced anticancer activity than that of the RV. As such, the novel synthetic compounds 3d, 3e and 3b endowed with potent anticancer activity than RV can serve as drug lead molecules.
authors.affiliation: CPMB, Osmania University, Hyderabad, 500007. India.
authors.forename: Raju
authors.initials: R
authors.lastname: Naini
authors.affiliation: Department of Biochemistry, Osmania University, Hyderabad. India.
authors.forename: Eslavath
authors.initials: E
authors.lastname: Ravikumar
authors.affiliation: Department of Biochemistry, Osmania University, Hyderabad. India.
authors.forename: Surya S
authors.initials: SS
authors.lastname: Singh
authors.affiliation: CPMB, Osmania University, Hyderabad, 500007. India.
authors.forename: Rama K
authors.initials: RK
authors.lastname: Kancha
authors.affiliation: CPMB, Osmania University, Hyderabad, 500007. India.
authors.forename: Khareedu V
authors.initials: KV
authors.lastname: Rao
authors.affiliation: CPMB, Osmania University, Hyderabad, 500007. India.
authors.forename: Vudem D
authors.initials: VD
authors.lastname: Reddy
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001682:Biological Availability; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D057809:HEK293 Cells; D006367:HeLa Cells; D006801:Humans; D007097:Imines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D007097:Imines; D013267:Stilbenes
keywords: HIF-1α; Imine stilbenes; analogs.; anti-cancer activity; cell motility; cell survival