Abstract
The series of 9,14-disubstituted 3,7-dithia-5,14-diazapentacyclo[9.5.1.02, 10.04, 8.012, 16]heptadecen-4(8)-triones-6, 13, 15 were synthesized using hetero-Diels-Alder reactions starting from 4-thioxo-2-thiazolidinones and 5-norbornene-2,3-dicarboxylic acid imido-derivatives. Screening of anticancer activity in vitro yielded the most active compounds 5c, 5d, and 7b in micromolar concentrations at the GI50 level (LogGI50 is−6.40 to−4.02 for different cell lines, LogGI50 mean graph midpoint varies from−4.67 to−4.05); moreover, compounds 5c and 5d have a distinctive selectivity against leukemia. The highest sensitivity to compound 5d showed leukemia cell lines CCRF-CEM (LogGI50=−6.40) and SR (LogGI50=−6.06).
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