Biopolymers and cell. 2003; 19 (3): 287 - 291

Search for antitumor activity among derivatives of the 2,5-dihydropyrrole-2,5-dione

S. S. Tarnavskiy, G. G. Dubinina, S. M. Golovach, S. M. Yarmoluk

39 derivatives of the 2,5-dihydropyrrole-2,5-dione were synthesized and tested on antitumor activity. The l-benzyl-3-chloro-4-(3-hydro-xyanilino)-2,5-dihydro-IH-2,5-pyrroledione (5.2) was selected after pre-screening and tested on 56 cell lines of human tumors. The compound 5.2 exhibits antitumor activity: CI₅₀ 2.68μM, LC₅₀ 31.7 μM (cell line MDA-MB-435 (Breast Cancer)); GI₅₀ 3.35 μM, LC₅₀ 37.6 μM (cell line OVCAR-3 (Ovarian Cancer)); GI₅₀ 6.75 μM, LC₅₀ 44.5 μM (cell line NCI-H23 (Non-small Cell Lung Cancer)).