79560-74-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of thiosemicarbazones, hydrazinobenzothiazoles and arylhydrazones as anticancer agents with a potential to overcome multidrug resistance
Pape, Veronika F.S.,Tóth, Szilárd,Füredi, András,Szebényi, Kornélia,Lovrics, Anna,Szabó, Pál,Wiese, Michael,Szakács, Gergely
, p. 335 - 354 (2016/05/19)
There is a constant need for new therapies against multidrug resistant (MDR) cancer. An attractive strategy is to develop chelators that display significant antitumor activity in multidrug resistant cancer cell lines overexpressing the drug efflux pump P-glycoprotein. In this study we used a panel of sensitive and MDR cancer cell lines to evaluate the toxicity of picolinylidene and salicylidene thiosemicarbazone, arylhydrazone, as well as picolinylidene and salicylidene hydrazino-benzothiazole derivatives. Our results confirm the collateral sensitivity of MDR cells to isatin-β-thiosemicarbazones, and identify several chelator scaffolds with a potential to overcome multidrug resistance. Analysis of structure-activity-relationships within the investigated compound library indicates that NNS and NNN donor chelators show superior toxicity as compared to ONS derivatives regardless of the resistance status of the cells.
THIOSEMICARBAZONES WITH MDR1 - INVERSE ACTIVITY
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Page/Page column 21; 37; 38, (2012/03/27)
Disclosed herein are drug compounds that have MDR-inverse activity and thus are effective against multidrug-resistant cells. Exemplary compounds disclosed herein have the structure;Formula (I). Examples of the disclosed compounds have been found to have,
Oxindole derivatives as inhibitors of TAK1 kinase
Lockman, Jeffrey W.,Reeder, Matthew D.,Robinson, Rosann,Ormonde, Patricia A.,Cimbora, Daniel M.,Williams, Brandi L.,Willardsen, J. Adam
scheme or table, p. 1724 - 1727 (2011/05/04)
Several series of oxindole analogues were synthesized and screened for inhibitory activity against transforming growth factor-β-activating kinase 1 (TAK1). Modifications around several regions of the lead molecules were made, with a distal hydroxyl group
Isatin-β-thiosemicarbazones as potent herpes simplex virus inhibitors
Kang, Iou-Jiun,Wang, Li-Wen,Hsu, Tsu-An,Yueh, Andrew,Lee, Chung-Chi,Lee, Yen-Chun,Lee, Ching-Yin,Chao, Yu-Sheng,Shih, Shin-Ru,Chern, Jyh-Haur
scheme or table, p. 1948 - 1952 (2011/05/04)
A series of isatin-β-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-β-thiosemicarbazone exhibited significant and selective antiviral activity with low cytotoxicity. It was found that the thiourea group at thiosemicarbazone and the NH functionality at isatin were essential for their antiherpetic activity. The synthesis and structure-activity relationship studies are presented.
Synthesis, activity, and pharmacophore development for isatin-β- thiosemicarbazones with selective activity toward multidrug-resistant cells
Hall, Matthew D.,Salam, Noeris K.,Hellawell, Jennifer L.,Fales, Henry M.,Kensler, Caroline B.,Ludwig, Joseph A.,Szakács, Gergely,Hibbs, David E.,Gottesman, Michael M.
experimental part, p. 3191 - 3204 (2010/03/31)
We have recently identified a new class of compounds that selectively kill cells that express P-glycoprotein (P-gp, MDR1), the ATPase efflux pump that confers multidrug resistance on cancer cells. Several isatin-β- thiosemicarbazones from our initial stud
Reactions of 3-Arylimino-2-Indolinones with p-Substituted Phenylthiosemicarbazides
Varma, Rajendra S.,Garg, Pradeep K.
, p. 980 - 981 (2007/10/02)
3-Arylimino-2-indolinones (II) have been prepared by the condensation of isatins (I) with anilines.Reactions of II with p-substituted phenylthiosemicarbazides have resulted (in every instance) in the displacement of arylimino groups by the phenylthiosemic
