Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities - Development of highly efficacious cytotoxic agents

Based upon the lead compounds 10 and 11, a number of conjugates were synthesized by the combination of chromone-pyrimidine, chromone-indolinone, chromone-pyrazole, indole-pyrimidine, indole-indolinone and indole-pyrazole moieties. Evaluation of these compounds for tumor growth inhibitory activities over 60 human tumor cell lines provided highly efficacious compounds 15, 41, 43, 66, 69, and 72 with an average GI(50) over all the 60 human tumor cell lines as 3.2 mu M, 3.1 mu M, 1.7 mu M, 2.6 mu M, 50.1 mu M and 2.0 mu M, respectively. (C) 2010 Elsevier Masson SAS. All rights reserved.