Both 5-arylidene-2-thioxodihydropyrimidine-4, 6 (1H, 5H)-diones and 3-thioxo-2, 3-dihydro-1H-imidazo [1, 5-a] indol-1-ones are light-dependent tumor necrosis factor- …

…, PH Carter, AJ Tebben, PA Scherle, GD Brown…

Index: Voss, Matthew E.; Carter, Percy H.; Tebben, Andrew J.; Scherle, Peggy A.; Brown, Gregory D.; Thompson, Lorin A.; Xu, Meizhong; Lo, Yvonne C.; Yang, Gengjie; Liu, Rui-Qin; Strzemienski, Paul; Everlof, J. Gerry; Trzaskos, James M.; Decicco, Carl P. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 3 p. 533 - 538

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Citation Number: 38

Abstract

Based on the realization that N-alkyl 5-arylidene-2-thioxo-1, 3-thiazolidin-4-ones are tumor necrosis factor-α antagonists, we discovered two additional classes of antagonists: 3-thioxo- 2, 3-dihydro-1H-imidazo [1, 5-a] indol-1-ones (via rational design) and 5-arylidene-2- thioxodihydropyrimidine-4, 6 (1H, 5H)-diones (via computer-guided screening). Chemical modification of the lead structures showed that the structure–activity relationship profiles ...