79560-73-9Relevant academic research and scientific papers
Isatin based thiosemicarbazide derivatives as potential inhibitor of α-glucosidase, synthesis and their molecular docking study
Hayat, Shawkat,Iqbal, Naveed,Khan, Khalid Mohammed,Nawaz, Muhammad,Qureshi, Faiza,Rab, Abdur,Rahim, Fazal,Shah, Syed Adnan Ali,Taha, Muhammad,Uddin, Imad,Uddin, Nizam,Wadood, Abdul,Zaman, Khalid
, (2020/07/25)
A new series of isatin based thiosemicarbazide derivatives 1–15 were synthesized and characterized by 1H NMR, 13C NMR and HR-EIMS. The synthetic derivatives were evaluated for α-glucosidase inhibitory potential. All compounds showed
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 44, (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,
Aqua mediated one pot facile synthesis of novel thioxo-1,2,4-triazin-5(2H)- one and [1,2,4] triazino[5,6-b]indole derivatives and their biological activities
Sachdeva, Harshita,Dwivedi, Diksha,Singh, Har Lal,Sharma, Kanti Prakash
, p. 1348 - 1354 (2013/06/27)
Rapid and highly efficient one pot green chemical synthesis of substituted 6-(2-aminophenyl)-4-(4-substitutedphenyl)-3-thioxo-3,4-dihydro-1,2, 4-triazin-5(2H)-one and 8-substituted-3,5-dihydro-2H-[1,2,4]triazino[5,6-b] indole is carried out in aqueous medium under microwave irradiation. Improved synthesis of potent bioactive Schiff and N-Mannich bases of hexahydro-1H-indole- 2,3-dione is also reported. The title compounds are easily accessible by various approaches; even waste free approaches have been developed. The operational simplicity, environmentally benign conditions and high yield achieved in a very short reaction time are major benefits that meet the requirements of green production, including saving energy and high efficiency. The results obtained under microwaves are compared with that of conventional heating. Structural assignments are based on spectroscopic data. Compounds have also been screened for antibacterial and antifungal activities.
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.
Syntheses of some substituted isatin-β-thiosemicarbazones and isatin-β-hydrazonothiazoline derivatives as potential antiviral and antimicrobial agents
Omar,Eshba,Salama
, p. 701 - 709 (2007/10/02)
A series of isatin-β-thioxemicarbazones and isatin-β-hydrazonothiazolines was synthesized by condensation of various isatin derivatives with N4-substituted-3-thiosemicarbazides and cyclization of the products by phenacyl bromides. The products
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
