Title of article :
design, synthesis and biological evaluation of 1,3-diphenyl-3-(phenylthio)propan-1-ones as new cytotoxic agents
Author/Authors :
bayanati, maryam shahid beheshti university of medical sciences - school of pharmacy - department of pharmaceutical chemistry, tehran, iran , shahhosseini, soraya shahid beheshti university of medical sciences - protein technology research center, tehran, iran , shirazi, farshad. h. shahid beheshti university of medical sciences - school of pharmacy - department of toxicology and pharmacology, tehran, iran , farnam, golrokh shahid beheshti university of medical sciences - school of pharmacy - department of toxicology and pharmacology, tehran, iran , zarghi, afshin shahid beheshti university of medical sciences - school of pharmacy - department of pharmaceutical chemistry, tehran, iran
Abstract :
cancers in terms of morbidity and mortality are one of the major universal issues. new compounds of anticancer agents based on β-aryl-β-mercapto ketones scaffold possessing piperidinylethoxy or morpholinylethoxy groups were synthesized and evaluated as cytotoxic agents. cytotoxic effects of synthesized compounds were measured against mcf-7, human erpositive breast cancer cell lines, using mtt assay. the results indicated that all compounds had high cytotoxic activity on mcf-7 cancerous cells, even more than the reference drug tamoxifen. among them, compounds 3-(4-(2-morpholinoethoxy)phenyl)-1-phenyl-3-(phenylthio) propan-1-one (4a) and 1-(4-methoxyphenyl)-3-(3-(2-morpholinoethoxy)phenyl)-3-(phenylthio)propan- 1-one (4h) had no significant cytotoxic effects on normal cells compared to tamoxifen. our results also indicated that adding tertiary amine basic side chain, found in tamoxifen drug, to 1,3-diphenyl-3-(phenylthio)propan-1-ones improves the cytotoxic effects of these compounds on breast cancer cells.
Keywords :
synthesis , 1,3 , diphenyl , 3 , (phenylthio)propan , 1 , one , docking study , cytotoxic effect , mtt , mcf , 7
Journal title :
Iranian Journal of Pharmaceutical Research(IJPR)
Journal title :
Iranian Journal of Pharmaceutical Research(IJPR)