Effects of a new antitumor compound, mopidamol, on thymidine and 2-deoxyglucose transport in leukaemic L 1210 cells.
The effects of 2,2',2",2"'-[(4-piperidinopyrimido[5,4-d]pyrimidine-2,6- diyl)dinitrilo]-tetraethanol (mopidamol, RA-233), a drug with antitumour properties, have been studied on membrane transports of L 1210 cells grown in culture. The results show that mopidamol is an inhibitor of thymidine and 2-deoxyglucose transport at concentrations less than or equal to 10(-4) mol/l. The inhibitory effect on cancer cells occurs as soon as 20 s after contact with the drug. Lineweaver and Burk's plots demonstrate a non-competitive type inhibitory effect on membrane transports. In addition, thymidine incorporation in DNA is decreased in the presence of mopidamol.
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002478:Cells, Cultured; D003837:Deoxy Sugars / Q000378:metabolism*; D003847:Deoxyglucose / Q000378:metabolism*; D007700:Kinetics; D007939:Leukemia L1210 / Q000378:metabolism*; D051379:Mice; D009012:Mopidamol / Q000494:pharmacology*; D011743:Pyrimidines / Q000494:pharmacology*; D013936:Thymidine / Q000378:metabolism*
D000970:Antineoplastic Agents; D003837:Deoxy Sugars; D011743:Pyrimidines; D009012:Mopidamol; D003847:Deoxyglucose; D013936:Thymidine