title: Novel Aza-resveratrol analogs: synthesis, characterization and anticancer activity against breast cancer cell lines.
abstract: Novel Aza-resveratrol analogs were synthesized, structurally characterized and evaluated for cytotoxic activity against MDA-MB-231 and T47D breast cancer cell lines, which exhibited superior inhibitory activity than parent resveratrol compound. The binding mechanism of these compounds with estrogen receptor-α was rationalized by molecular docking studies which indicated additional hydrogen binding interactions and tight binding in the protein cavity. Induction of Beclin-1 protein expression in breast cancer cell lines after treatment with newly synthesized resveratrol analogs indicated inhibition of growth of these cell lines through autophagy. The study highlighted the advantage of introducing the imino-linkage in resveratrol motif in enhancing the anticancer potential of resveratrol suggesting that these analogs can serve as better therapeutic agents against breast cancer and can provide starting point for building more potent analogs in future.
authors.affiliation: ISTRA, MCES's Allana College of Pharmacy, University of Pune, India.
authors.forename: Areej
authors.initials: A
authors.lastname: Siddiqui
authors.forename: Prasad
authors.initials: P
authors.lastname: Dandawate
authors.forename: Rukhsana
authors.initials: R
authors.lastname: Rub
authors.forename: Subhash
authors.initials: S
authors.lastname: Padhye
authors.forename: Shama
authors.initials: S
authors.lastname: Aphale
authors.forename: Alpana
authors.initials: A
authors.lastname: Moghe
authors.forename: Amrit
authors.initials: A
authors.lastname: Jagyasi
authors.forename: K
authors.initials: K
authors.lastname: Venkateswara Swamy
authors.forename: Bhupendra
authors.initials: B
authors.lastname: Singh
authors.forename: Anwesha
authors.initials: A
authors.lastname: Chatterjee
authors.forename: Amruta
authors.initials: A
authors.lastname: Ronghe
authors.forename: Hari K
authors.initials: HK
authors.lastname: Bhat
mesh_terms: D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003198:Computer Simulation; D047628:Estrogen Receptor alpha / Q000378:metabolism*; D005260:Female; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D006860:Hydrogen Bonding; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding / Q000187:drug effects; D000077185:Resveratrol; D013267:Stilbenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D001372:Aza Compounds; C506487:ESR1 protein, human; D047628:Estrogen Receptor alpha; D013267:Stilbenes; D000077185:Resveratrol