28492-94-6Relevant articles and documents
Electrochemical characterization of isatin-thiosemicarbazone derivatives
Bandeira, Katlen Christian Tribuzy,Bohs, Lucas Martins Correa,Bresolin, Leandro,Gervini, Vanessa Carratu,Godoi, Marcelo,Justim, Juliano da Rosa,Martins, Bianca Barreto,Melo, Ana Paula Lopes de,Peixoto, Carlos Roberto de Menezes
, (2021/11/26)
Abstract: Herein, we have notably described the electrochemical behavior of four isatin-thiosemicarbazone derivatives. In this regard, cyclic voltammograms of isatin-3-thiosemicarbazone (ITSC), isatin-3-(N4-benzylthiosemicarbazone) (ITSC-Ph), 1-(5-nitro-2-oxoindolin-3-ylidene)thiosemicarbazide (NO2-ITSC) and 1-(5-nitro-2-oxoindolin-3-ylidene)-4-phenylthiosemicarbazide (NO2-ITSC-Ph) have demonstrated an irreversible oxidation process. More specifically, the generation of isatin and thiourea moieties as the final oxidation products was proposed. The cyclic voltammograms also demonstrate irreversible reduction processes of ITSC and ITSC-Ph in three steps. The proposed final products are 3-aminoindolin-2-one and thiourea moieties. In the cyclic voltammograms of NO2-ITSC and NO2-ITSC-Ph, five reduction processes were observed: three of them due to reduction of the nitro group. It was proposed that the formation of 5-hydroxyamino-3-iminoindolin-2-one and the thiourea moieties would be the final products. Graphic abstract: [Figure not available: see fulltext.] Electrochemical characterization of four isatin thiosemicarbazone derivatives is described. The compounds are irreversibly oxidized and reduced. Isatin moieties and thiourea are proposed to be the products generated after oxidation. Considering the reduction processes, the nitro group present at the isatin moiety is also reduced and influences the reduction products generated.
Insight on a new indolinone derivative as an orally bioavailable lead compound against renal cell carcinoma
Fouad, Marwa A.,Zaki, Mayssoune Y.,Lotfy, Raghda A.,Mahmoud, Walaa R.
, (2021/06/15)
A series of novel 3-indolinone-thiazolidinones and oxazolidinones 4a-k was synthesized via molecular hybridization approach and sequentially evaluated to explore its cytotoxic activity. The cytotoxicity screening pointed toward the N-cyclohexyl thiazolidinone derivative 4f that revealed promising renal cytotoxicity against CAKI-1 and UO-31 renal cancer cell lines with IC50 values 4.74 and 3.99 μM, respectively, which were comparable to those of sunitinib along with good safety threshold against normal renal cells. Further emphasis on compound 4f renal cytotoxicity was achieved via different enzyme assays and CAKI-1 and UO-31 cell cycle analysis. The results were supported by in silico studies to explore its physicochemical, pharmacokinetic and drug-likeness properties. Finally, compound 4f was subjected to an in vivo pharmacokinetic study through two different routes of administration showing excellent oral bioavailability. This research represents compound 4f as a promising candidate against renal cell carcinoma.
First identification of isatin-β-thiosemicarbazones as novel inhibitors of New Delhi metallo-β-lactamase-1: Chemical synthesis, biological evaluation and molecular simulation
Song, Guo-Qing,Wang, Wei-Min,Li, Zai-Shun,Wang, Ying,Wang, Jian-Guo
, p. 899 - 902 (2017/10/06)
New Delhi metallo-β-lactmase-1 (NDM-1) catalyzes the hydrolysis of β-lactam antibiotics and cleaves the β-lactam ring of the molecule, conferring bacterial resistance against these medicines. In an effort to discover novel agents to treat this superbug, a
