Quantitative structure-activity relationships (QSAR) have been formulated for the hydrolysis of aniline mustards and their antitumor activity against Walker 256 tumor and L1210 and P388 leukemia. In general, the antitumor activity parallels hydrolysis under the conditions defined by Ross; toxicity (LD50) parallels antitumor efficacy. Chlorambucil is an exception. A most important finding is that ideal lipophilicity for effectiveness against Walker tumor appears to be much higher than for the leukemias which suggests that solid tumors may, in general, require more lipophilic drugs than leukemias.
Jonathan R. Dimmock, N. Murthi Kandepu, Mark Hetherington, J. Wilson Quail, U. Pugazhenthi, Athena Sudom, Mahmood Chamankhah, Patricia A. Rose, Eric W. Pass, Theresa M. Allen, S. Halleran, Jen Szydlowski, Bülent Mutus, Marie Tannous, Elias K. Manavathu, Timothy G. Myers, De Clercq Erik, Jan Balzarini
Tatjana Gazivoda, Mario Šokčević, Marijeta Kralj, Lidija Šuman, Krešimir Pavelić, De Clercq Erik, Graciela Andreï, Robert Snoeck, Jan Balzarini, Mladen Mintas, Silvana Raić‐Malić
Discussion(0)
No comments yet. Be the first to comment.