- Synthesis, structures, antimicrobial activity and biosafety evaluation of pyridine-2-formaldehyde-N-susbtituted-thiosemicarbazonates of copper(ii)
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Pyridine-2-formaldehyde-N1-substituted-thiosemicarbazones {(C5H4N4)HC2═N3-N2(H)-C1═(S)N1HR} (abbrev. HL1-R: R = Me, Et, Ph) with copper(i) halides in an acetonitrile-dichloromethane mixture (1?:?1, v/v) have yielded a novel series of CuII complexes with a central coordination core: [CuIIX(N,N,S-L1-R)] (R = Me, Et, Ph: X = I, 1-3; Br, 4-6, Cl, 7-9), which have been characterized with the help of analytical data, IR, UV-visible and ESR spectroscopy, ESI-mass spectrometry and single crystal X-ray crystallography. The thio-ligands coordinate to CuII as anions (L1-R)? through pyridyl nitrogen-N4, azomethine nitrogen-N3 and thiolato sulfur and CuII is further bonded to iodide, bromide or chloride. In order to explore their bio-activity, complexes (1-9) as well as the previously reported CuII complexes of 2-benzoylpyridine-N-substituted thiosemicarbazones {(C5H4N4)(C6H5)-C2═N3-N2(H)-C1═(S)-N1HR; HL2-R}, namely, [CuIIX(N,N,S-L2-R)] (R = Me, Et, Ph: X = I, 10-12; Br, 13-15; Cl, 16-18), have been evaluated for their antimicrobial potential against different microbial strains. The microbial strains investigated are Staphylococcus aureus (MTCC740), Klebsiella pneumoniae (MTCC530), Shigella flexneri (MTCC1457), Salmonella typhimurium 1 (MTCC98), Salmonella typhimurium 2 (MTCC1251), Escherichia coli (MTCC119), Staphylococcus epidermidis (MTCC435), methicillin resistant Staphylococcus aureus (MRSA) and a yeast culture Candida albicans (MTCC227). Several complexes tested have shown high antimicrobial activity; specifically, against methicillin resistant Staphylococcus aureus, Staphylococcus epidermidis and Salmonella typhimurium 2; the activity is found to be high at low minimum inhibitory concentration (MIC) values as compared to that of the standard Gentamicin. Using MTT cytotoxicity assay {MTT = 3-[(4,5-dimethylthiazol-2-yl)-2,5-diphenyl]tetrazolium bromide}, complexes tested were found to be biosafe with high cell viability (90-98%).
- Kaushal, Mani,Lobana, Tarlok S.,Nim, Lovedeep,Kaur, Jaskamal,Bala, Ritu,Hundal, Geeta,Arora, Daljit S.,Garcia-Santos, Isabel,Duff, Courtney E.,Jasinski, Jerry P.
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- Developing a Novel Indium(III) Agent Based on Liposomes to Overcome Cisplatin-Induced Resistance in Breast Cancer by Multitargeting the Tumor Microenvironment Components
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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
- Chu, Yong,Jiang, Ming,Li, Wenjuan,Liang, Hong,Sun, Hongbin,Yang, Feng,Yang, Tongfu,Zhang, Zhenlei
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p. 14587 - 14602
(2021/10/25)
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- FTO small molecule inhibitor palladium complex and synthesis method thereof
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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
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Paragraph 0009; 0034-0037
(2020/11/26)
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- Indium compound taking 2-pyridylaldehyde thiosemicarbazone as ligand as well as synthesis method and application thereof
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The invention discloses an indium compound taking 2-pyridylaldehyde thiosemicarbazone as a ligand as well as a synthesis method and application thereof. The synthesis method comprises the following steps: dissolving thiosemicarbazide into methanol; after
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Paragraph 0043-0046
(2019/06/12)
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- Platinum complex taking 2-pyridine formaldehyde thiosemicarbazone as ligand and synthesis method and application thereof
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The invention discloses a platinum complex taking 2-pyridine formaldehyde thiosemicarbazone as ligand and a synthesis method and application thereof. The synthesis method includes: dissolving thiosemicarbazone in methanol, adding 2-pyridylaldehyde after d
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Paragraph 0041-0044
(2019/07/01)
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- Designing anticancer copper(II) complexes by optimizing 2-pyridine-thiosemicarbazone ligands
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To develop potential next-generation metal anticancer agents, we designed and synthesised five Cu(II) 2-pyridine-thiosemicarbazone complexes by modifying the hydrogen atom at the N-4 position of ligands, and then investigated their structure-activity rela
- Deng, Jungang,Yu, Ping,Zhang, Zhenlei,Wang, Jun,Cai, Jinhua,Wu, Na,Sun, Hongbin,Liang, Hong,Yang, Feng
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p. 442 - 452
(2018/09/22)
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- Synthesis of four binuclear copper(II) complexes: Structure, anticancer properties and anticancer mechanism
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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
- Qi, Jinxu,Liang, Shichu,Gou, Yi,Zhang, Zhenlei,Zhou, Zuping,Yang, Feng,Liang, Hong
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p. 360 - 368
(2015/04/27)
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- Role of Metalation in the Topoisomerase IIα inhibition and antiproliferation activity of a series of α-heterocyclic-N 4-substituted thiosemicarbazones and their Cu(II) complexes
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The topoisomerase-IIα inhibition and antiproliferative activity of α-heterocyclic thiosemicarbazones and their corresponding copper(II) complexes have been investigated. The CuII(thiosemicarbazonato)Cl complexes were shown to catalytically inhi
- Zeglis, Brian M.,Divilov, Vadim,Lewis, Jason S.
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experimental part
p. 2391 - 2398
(2011/06/10)
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