3608-75-1Relevant academic research and scientific papers
Transition metal complexes of 2-formylpyridinethiosemicarbazone (HFpyTSC) and X-ray crystal structures of [Pd(FpyTSC)(PPh3)]PF6and [Pd(FpyTSC)(SCN)]
Elsayed, Shadia A.,El-Hendawy, Ahmed M.,Mostafa, Sahar I.,Butler, Ian S.
, p. 2526 - 2532 (2010)
The syntheses of five new complexes of the 2- formylpyridinethiosemicarbazone ligand (HFpyTSC) with Pd(II) and Rh(III) ions are described, viz., [Pd(FpyTSC)(PPh3)]PF6, [Pd(FpyTSC)(SCN)], [Pd(FpyTSC)Br], [Pd(HFpyTSC)2]Brsu
Novel pyridinecarboxaldehyde thiosemicarbazone conjugated magnetite nanoparticulates (MNPs) promote apoptosis in human lung cancer A549 cells
Habibi, Alireza,Sadat Shandiz, Seyed Ataollah,salehzadeh, Ali,Moradi-Shoeili, Zeinab
, p. 13 - 22 (2020)
The present study highlights the apoptotic activity of magnetic Fe3O4 nanoparticulates functionalized by glutamic acid and 2-pyridinecarboxaldehyde thiosemicarbazone (PTSC) toward human lung epithelial carcinoma A549 cell line. To this aim, the Fe3O4 nanoparticulates were prepared using co-precipitation method. Then, the glutamic acid and Fe3O4 nanoparticulates were conjugated to each other. The product was further functionalized with bio-reactive PTSC moiety. In addition, the synthesized Fe3O4@Glu/PTSC nanoparticulates were characterized by physico-chemical techniques including scanning electron microscope (SEM), energy dispersive X-ray (EDX), X-ray diffraction (XRD), Fourier-transform infrared (FT–IR) spectroscopy and zeta potential analysis. The effects of in vitro cell viability in Fe3O4@Glu/PTSC nanoparticulate indicated the anti-proliferative properties in a dose-dependent manner (IC50 = 135.6?μM/mL). The high selectivity for tumor cells and far below of activity in HEK293 non-tumorigenic cells is considered as an important feature for this complex (SI, 3.48). Based on the results, PTSC failed to reveal any activity against A549 cells alone. However, Fe3O4 nanoparticulates had some effects in inhibiting the growth of lung cancer cell. Furthermore, Bax and Bcl-2 gene expressions were quantified by real-time PCR method. The expression of Bax increased 1.62-fold, while the expression of Bcl-2 decreased 0.76-fold at 135.6?μM/mL concentration of Fe3O4@Glu/PTSC compared to untreated A549 cells. Furthermore, the Fe3O4@Glu/PTSC nanoparticulate-inducing apoptosis properties were evaluated by Hoechst 33258 staining, Caspase-3 activation assay and Annexin V/propidium iodide staining. The results of the present study suggest that Fe3O4@Glu/PTSC nanoparticulates exhibit effective anti-cancer activity against lung cancer cells.
Spectroscopic and biological approach of Ni(II) and Cu(II) complexes of 2-pyridinecarboxaldehyde thiosemicarbazone
Chandra, Sulekh,Raizada, Smriti,Tyagi, Monika,Sharma, Praveen Kumar
, p. 816 - 821 (2008)
Ni(II) and Cu(II) complexes having the general composition [M(L)2X2] [where L = 2-pyridinecarboxaldehyde thiosemicarbazone, M = Ni(II) and Cu(II), X = Cl-, NO3- and 1/2 SO42-] have been synthesized. All the metal complexes were characterized by elemental analysis, molar conductance, magnetic moment, mass, IR, EPR and electronic spectral studies. The magnetic moment measurements of the complexes indicate that all the complexes are of high-spin type. On the basis of spectral studies an octahedral geometry has been assigned for Ni(II) complexes whereas tetragonal geometry for Cu(II) except [Cu(L)2SO4] which posseses five coordinated geometry. The ligand and its metal complexes were screened against phytopathogenic fungi and bacteria in vitro.
Synthesis of four binuclear copper(II) complexes: Structure, anticancer properties and anticancer mechanism
Qi, Jinxu,Liang, Shichu,Gou, Yi,Zhang, Zhenlei,Zhou, Zuping,Yang, Feng,Liang, Hong
, p. 360 - 368 (2015)
Four binuclear Cu(II)-Schiff base complexes were synthesized and characterized.Cu complexes have high anticancer activity.Cu complexes induce cells apoptosis possible via intrinsic ROS-mediated mitochondrial pathway.Cu complexes regulate Bcl-2 family prot
A multi-responsive thiosemicarbazone-based probe for detection and discrimination of group 12 metal ions and its application in logic gates
Sarkar, Soma,Mondal, Tapashree,Roy, Swapnadip,Saha, Rajnarayan,Ghosh, Ashish Kumar,Panja, Sujit S.
, p. 15157 - 15169 (2018)
A new simple 3-in-1 multi-response thiosemicarbazone-based chemosensor has been synthesized and characterized. The probe not only exhibited high sensitivity towards the most familiar and abundant group 12 metal ions, viz., Zn2+, Cd2+ and Hg2+, in MeCN-H2O (1 : 1, v/v) medium but also can efficiently distinguish them through significant changes in their absorption and emission spectral behavior. The selectivity response was found to follow the order Hg2+, Cd2+, Zn2+ due to the different degrees of stability of their respective complexes, which was further established by TDDFT calculations and interference studies. The binding affinities of the probe towards these metal ions were investigated by absorption, fluorescence emission, fluorescence lifetime, mass spectral and 1H NMR spectral measurements. The effects of solvent polarity on the probe molecule were also examined. Due to the observation of different binding affinities and the ensuing significant changes in absorbance at different wavelengths by a combination of different inputs, L can be judiciously applied for the construction of some basic logic gates (AND, OR, NOT, IMPLICATION and INHIBIT).
Developing a Novel Indium(III) Agent Based on Liposomes to Overcome Cisplatin-Induced Resistance in Breast Cancer by Multitargeting the Tumor Microenvironment Components
Chu, Yong,Jiang, Ming,Li, Wenjuan,Liang, Hong,Sun, Hongbin,Yang, Feng,Yang, Tongfu,Zhang, Zhenlei
, p. 14587 - 14602 (2021/10/25)
To overcome the resistance of cancer cells to platinum-based drugs and effectively suppress tumor growth, we developed a novel indium (In) agent based on liposomes (Lips). Thus, we not only obtained an In(III) thiosemicarbazone agent (5b) with remarkable
Development of a multi-target anticancer Sn(ii) pyridine-2-carboxaldehyde thiosemicarbazone complex
Li, Wenjuan,Liang, Hong,Pang, Min,Sun, Hongbin,Wang, Xiaojun,Wu, Junmiao,Yang, Feng,Yang, Tongfu
, p. 10909 - 10921 (2021/08/17)
In this study, we proposed to design effective multi-target anticancer agents based on the chelation of nontoxic metals with ligands that possess anticancer activity. In total, five Sn(ii) pyridine-2-carboxaldehyde thiosemicarbazone complexes are synthesi
Design and efficient synthesis of novel 4,5-dimethylthiazole-hydrazone derivatives and their anticancer activity
Evren, Asaf Evrim,Yurtta?, Leyla,Ekselli, Bü?ra,Aksoy, Onur,Akalin-?ift?i, Gül?en
, p. 372 - 386 (2021/06/17)
Background: Recently, researchers have been warning about the increased mortality of the various cancer types. Also, the lung adenocarcinoma and the glioma types are burning issues for world's health due to late or wrong diagnosis and/or insufficient treatment methods. For this purpose, our research group designed and synthesized novel 4,5-dimethyl thiazole-hydrazone derivatives which were tested against cancer and normal cell lines to understand the structure-activity relationship (SAR). Methods: The lead compounds were obtained by reacting 2-(substituted aryl-2-ylmethylene) hydrazin-1-carbothioamide with 3-chloro-2-butanone derivatives. The structural elucidation of the compounds was performed by1H-NMR,13C-NMR, and LC/MS-IT-TOF spectral and elemental analyses. The synthesized compounds were tested in vitro for the anticancer activity against A549 human lung adenocarcinoma and C6 rat glioma cells and investigated for which pathway to induce cell death. Also, the docking study of the active compounds was achieved to understand the SAR. Results: The targeted compounds (2a-2l) were synthesized successfully above 70% yields, and the analysis findings proved their purity. In general, the results of activity studies displayed significant effects against at least one cell line, except compounds 2e (indol-3-yl) and 2h (4-dimethylaminophenyl). Furthermore, compounds 2b and 2f displayed potential anticancer activity. With the help of molecular docking study, a potential selectivity of compound 2f was observed for type II protein kinase. On the other hand, compound 2b interacted with the active site nearly the same as Dasatinib. Therefore, these two compounds could be used as a base on developing selective anticancer drugs. Conclusion: Pyridin-2-yl (2b) derivative was found to be a favorable molecule with high anticancer potency against C6 and A549 cell lines. Additionally, 1-naphthyl (2f) derivative was a worthy compound for potential selectivity. In future studies, it will be our priority to focus on developing derivatives of these two compounds (2b and 2f) and elucidate their mechanisms.
Thiosemicarbazones exhibit inhibitory efficacy against New Delhi metallo-β-lactamase-1 (NDM-1)
Ge, Ying,Kang, Peng-Wei,Li, Jia-Qi,Gao, Han,Zhai, Le,Sun, Le-Yun,Chen, Cheng,Yang, Ke-Wu
, p. 574 - 579 (2021/07/17)
The superbug infection caused by metallo-β-lactamases (MβLs) carrying drug-resistant bacteria, specifically, New Delhi metallo-β-lactamase (NDM-1) has become an emerging threat. In an effort to develop novel inhibitors of NDM-1, thirteen thiosemicarbazones (1a-1m) were synthesized and assayed. The obtained molecules specifically inhibited NDM-1, with an IC50 in the range of 0.88–20.2 μM, and 1a and 1f were found to be the potent inhibitors (IC50 = 1.79 and 0.88 μM) using cefazolin as substrate. ITC and kinetic assays indicated that 1a irreversibly and non-competitively inhibited NDM-1 in vitro. Importantly, MIC assays revealed that these molecules by themselves can sterilize NDM-producing clinical isolates EC01 and EC08, exhibited 78-312-fold stronger activities than the cefazolin. MIC assays suggest that 1a (16 μg ml?1) has synergistic antimicrobial effect with ampicillin, cefazolin and meropenem on E. coli producing NDM-1, resulting in MICs of 4-32-, 4-32-, and 4-8-fold decrease, respectively. These studies indicate that the thiosemicarbazide is a valuable scaffold for the development of inhibitors of NDM-1 and NDM-1 carrying drug-resistant bacteria.
FTO small molecule inhibitor palladium complex and synthesis method thereof
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Paragraph 0009; 0028-0031, (2020/11/26)
The invention discloses an FTO small molecule inhibitor palladium complex and a synthesis method thereof. The synthesis method comprises the following steps: dissolving thiosemicarbazide in anhydrousCH3OH, then adding 2-pyridylaldehyde, carrying out reflu
