title: Synthesis, aerobic cytotoxicity, and radiosensitizing activity of novel 2,4-dinitrophenylamine tethered 5-fluorouracil and hydroxyurea.
abstract: Two novel dual functional agents, 3[3-(2,4-dinitro-phenylamino)-propyl]-5-fluoro-1H-pyrimidine-2,4-dione 7 and N-[3-(2,4-dinitro-phenylamino)-propoxy]urea 8, resulting from linkage of 2,4-dinitrophenylamine through three carbon atoms with 5-fluorouracil 5 and hydroxyurea 6, respectively, were prepared and their in vitro aerobic cytotoxicities in HT-29 cell line with and without radiation were determined. Compounds 7 and 8 unlike their components were not cytotoxic but showed radiosensitizing activity.
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14174, Iran. khalaj@ams.ac.ir <khalaj@ams.ac.ir>
authors.forename: Ali
authors.initials: A
authors.lastname: Khalaj
authors.forename: Ali Reza
authors.initials: AR
authors.lastname: Doroudi
authors.forename: Seyed Nasser
authors.initials: SN
authors.lastname: Ostad
authors.forename: Mohammad Reza
authors.initials: MR
authors.lastname: Khoshayand
authors.forename: Mohammad
authors.initials: M
authors.lastname: Babai
authors.forename: Neda
authors.initials: N
authors.lastname: Adibpour
mesh_terms: D000332:Aerobiosis; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D005472:Fluorouracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D019073:HT29 Cells; D006801:Humans; D006918:Hydroxyurea / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D015394:Molecular Structure; D009574:Nitro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D011838:Radiation-Sensitizing Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D013329:Structure-Activity Relationship
chemical_list: D009574:Nitro Compounds; D011838:Radiation-Sensitizing Agents; D005472:Fluorouracil; D006918:Hydroxyurea