13431-34-0Relevant articles and documents
A hydrazine-based thiocarbamide probe for colorimetric and turn-on fluorometric detection of PO43- and AsO33- in semi-aqueous medium
Purkait, Rakesh,Maity, Suvendu,Sinha, Chittaranjan
, p. 6236 - 6246 (2018)
2,6-Bis(N-ethylhydrazonethiocarbamide)-4-methyl-phenol (HTP) recognizes PO43- and AsO33- and is effective as a colorimetric and turn-on fluoremetric sensor in the presence of a large number of biologically impor
A novel 8-nitro quinoline-thiosemicarbazone analogues induces G1/S & G2/M phase cell cycle arrest and apoptosis through ROS mediated mitochondrial pathway
Arasakumar, Thangaraj,Athimoolam, Shunmuganarayanan,Mohan, Palathurai Subramaniam,Saravanan, Arjunan,Shyamsivappan, Selvaraj,Suresh, Thangaraj,Vivek, Raju
, (2020)
A series of novel 8-nitro quinoline-based thiosemicarbazone analogues were synthesized and characterized by various spectroscopic and single crystal X-ray analyses. The potent antitumor effects of synthesized compounds towards the cancer cells were evaluated by MTT assay. Amongst, the compound 3a exhibited the highest inhibitory activity and the compounds 3f and 3b were also showed significant activity. The molecular mechanistic studies of cell death have demonstrated that the treated potent compound 3a induced G1/S & G2/M phase cell cycle arrest and induced apoptosis via mitochondrial dysfunction and increased the production of cytotoxic ROS levels. The RT-PCR gene expression analysis revealed that the cell death induced by activation of caspase-3 dependent intrinsic apoptotic signaling pathway. Further, the molecular binding affinity of compounds with estrogen receptor alpha was calculated by molecular docking studies. Thus, novel 8-nitro quinoline-thiosemicarbazone analogues provide a unique tool for breast cancer therapeutic tactics.
Insight on a new indolinone derivative as an orally bioavailable lead compound against renal cell carcinoma
Fouad, Marwa A.,Lotfy, Raghda A.,Mahmoud, Walaa R.,Zaki, Mayssoune Y.
, (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.
Novel thiosemicarbazone derivatives: In vitro and in silico evaluation as potential mao-b inhibitors
?zkay, Yusuf,Kaplanc?kl?, Zafer As?m,Kurban, Berkant,Levent, Serkan,Osmaniye, Derya,Sa?l?k, Begüm Nurpelin
, (2021/11/11)
MAO-B inhibitors are frequently used in the treatment of neurodegenerative diseases such as Parkinson’s and Alzheimer’s. Due to the limited number of compounds available in this field, there is a need to develop new compounds. In the recent works, it was shown that various thiosemicarbazone derivatives show hMAO inhibitory activity in the range of micromolar concen-tration. It is thought that benzofuran and benzothiophene structures may mimic structures such as indane and indanone, which are frequently found in the structures of such inhibitors. Based on this view, new benzofuran/benzothiophene and thiosemicarbazone hybrid compounds were synthesized, characterized and screened for their hMAO-A and hMAO-B inhibitory activity by an in vitro fluorometric method. The compounds including methoxyethyl substituent (2b and 2h) were found to be the most effective agents in the series against MAO-B enzyme with the IC50 value of 0.042 ± 0.002 μM and 0.056 ± 0.002 μM, respectively. The mechanism of hMAO-B inhibition of compounds 2b and 2h was investigated by Lineweaver–Burk graphics. Compounds 2b and 2h were reversible and non-competitive inhibitors with similar inhibition features as the substrates. The Ki values of compounds 2b and 2h were calculated as 0.035 μM and 0.046 μM, respectively, with the help of secondary plots. The docking study of compound 2b and 2h revealed that there is a strong interaction between the active sites of hMAO-B and analyzed compound.
