192996-35-3Relevant academic research and scientific papers
Structure-based design of new poly (ADP-ribose) polymerase (PARP-1) inhibitors
Chadha, Navriti,Jaggi, Ameteshar Singh,Silakari, Om
, p. 655 - 660 (2017)
Poly (ADP-ribose) polymerase (PARP-1) is a well-established nuclear protein with prominent role in signaling and DNA repair. Various clinical candidates have been identified with the role in PARP-1 inhibition. Based on the pharmacophoric features identified from previous studies and molecular docking interactions, thiazolidine-2,4-dione derivatives have been evaluated for their PARP inhibitory activity. From an in vitro assay, 5-((1-(4-isopropylbenzyl)-1H-indol-3-yl)methylene)thiazolidine-2,4-dione (16) was identified as a potent inhibitor having low micromolar inhibitory activity (IC50=0.74±0.25μM). Thus, a structure-based design approach utilized in the present study helped to identify thiazolidine-2,4-dione as a novel scaffold against PARP-1 for potential development of potent anticancer therapeutics.
Novel, recyclable, and thermally stable task-specific ionic liquid (TBA acetate) medium/catalyst for the synthesis of indolylidinecyclic-1,3- and -1,4-diketones
Riyaz, Sd.,Indrasena,Naidu,Dubey
, p. 368 - 373 (2014/01/06)
A simple and efficient synthesis of indolylidinethiazolidnediones (3) and indolylidinecyclic-1,3-diketones (5) has been developed by reaction of indole-3-aldehyde (1) with thiazolidinedione (2) or cyclic-1,3-diketones (4) using tetra butyl ammonium acetat
L-proline-catalyzed synthesis of novel 5-(1H-indol-3-yl-methylene)- thiazolidine-2,4-dione derivatives as potential antihyperglycemic agents
Riyaz,Naidu,Dubey
experimental part, p. 2756 - 2762 (2011/09/15)
Knoevenagel condensation between indole-3-aldehyde 1 and an active methylene group containing 2,4-thiazolidinedione 2 in refluxing toluene using L-proline as a catalyst yielded 3, which on alkylation using 2 equivalents of alkylating agent under phase-tra
