Synthesis, aerobic cytotoxicity, and radiosensitizing activity of novel 2,4-dinitrophenylamine tethered 5-fluorouracil and hydroxyurea.
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.
Khalaj
Ali
A
Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14174, Iran. khalaj@ams.ac.ir <khalaj@ams.ac.ir>
Doroudi
Ali Reza
AR
Ostad
Seyed Nasser
SN
Khoshayand
Mohammad Reza
MR
Babai
Mohammad
M
Adibpour
Neda
N
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
D009574:Nitro Compounds; D011838:Radiation-Sensitizing Agents; D005472:Fluorouracil; D006918:Hydroxyurea