- Novel salicyloylhydrazone derivatives and corresponding terbium(III) complexes: Synthesis and properties research
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Four novel salicyloylhydrazone derivatives and their terbium(III) complexes were synthesized and characterized. The thermal analysis results showed that the terbium(III) complexes possessed good thermal stability. The fluorescence research results showed that the terbium(III) complex substituted by phenyl possessed the best fluorescence intensity among them, and its fluorescence quantum yield was also the highest. The exploration of the electrochemical properties indicated that the introduction of electron-donating groups to the ligand can increase the highest occupied molecular orbital (HOMO) energy levels and decrease the oxidation potential of the corresponding terbium(III) complexes. The introduction of electron-withdrawing groups to the ligand can reduce their HOMO energy levels and increase their oxidation potential. The results showed that the terbium(III) complexes are good candidates for luminescent material.
- Xiao, Rong,Huang, Wei,Xiao, Xiaoming,Liu, Yanhong,Guo, Dongcai
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- Discovery of an Orally Efficacious MYC Inhibitor for Liver Cancer Using a GNMT-Based High-Throughput Screening System and Structure-Activity Relationship Analysis
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Glycine-N-methyl transferase (GNMT) downregulation results in spontaneous hepatocellular carcinoma (HCC). Overexpression of GNMT inhibits the proliferation of liver cancer cell lines and prevents carcinogen-induced HCC, suggesting that GNMT induction is a potential approach for anti-HCC therapy. Herein, we used Huh7 GNMT promoter-driven screening to identify a GNMT inducer. Compound K78 was identified and validated for its induction of GNMT and inhibition of Huh7 cell growth. Subsequently, we employed structure-activity relationship analysis and found a potent GNMT inducer, K117. K117 inhibited Huh7 cell growth in vitro and xenograft in vivo. Oral administration of a dosage of K117 at 10 mpk (milligrams per kilogram) can inhibit Huh7 xenograft in a manner equivalent to the effect of sorafenib at a dosage of 25 mpk. A mechanistic study revealed that K117 is an MYC inhibitor. Ectopic expression of MYC using CMV promoter blocked K117-mediated MYC inhibition and GNMT induction. Overall, K117 is a potential lead compound for HCC- and MYC-dependent cancers.
- Kant, Rajni,Yang, Ming-Hui,Tseng, Chih-Hua,Yen, Chia-Hung,Li, Wei-You,Tyan, Yu-Chang,Chen, Marcelo,Tzeng, Cherng-Chyi,Chen, Wei-Cheng,You, Kaiting,Wang, Wen-Chieh,Chen, Yeh-Long,Chen, Yi-Ming Arthur
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p. 8992 - 9009
(2021/07/19)
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- Synthesis, Characterization and Crystal Structures of Cobalt(II), Zinc(II) and Cadmium(II) Complexes Derived from 2-Hydroxy-N’-(pyridin-2-ylmethylene)benzohydrazide with Antimicrobial Activity
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Three new cobalt(II), zinc(II) and cadmium(II) complexes, [CoL2] · 2CH3OH · H2O (1), [ZnL2] (2) and [Cd(HL)2(NO3)] N3 (3), were prepared from 2-hydroxy-N’-(pyridin-2-ylmethylene)
- Wang, Li-Hang,Qiu, Xiao-Yang,Liu, Shu-Juan
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p. 675 - 680
(2019/10/14)
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- Potent antimicrobial agents against azole-resistant fungi based on pyridinohydrazide and hydrazomethylpyridine structural motifs
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Abstract Schiff base derivatives have recently been shown to possess antimicrobial activity, and these derivatives include a limited number of salicylaldehyde hydrazones. To further explore this structure-activity relationship between salicylaldehyde hydrazones and antifungal activity, we previously synthesized and analyzed a large series of salicylaldehyde and formylpyridinetrione hydrazones for their ability to inhibit fungal growth of both azole-susceptible and azole-resistant species of Candida. While many of these analogs showed excellent growth inhibition with low mammalian cell toxicity, their activity did not extend to azole-resistant species of Candida. To further dissect the structural features necessary to inhibit azole-resistant fungal species, we synthesized a new class of modified salicylaldehyde derivatives and subsequently identified a series of modified pyridine-based hydrazones that had potent fungicidal antifungal activity against multiple Candida spp. Here we would like to present our synthetic procedures as well as the results from fungal growth inhibition assays, mammalian cell toxicity assays, time-kill assays and synergy studies of these novel pyridine-based hydrazones on both azole-susceptible and azole-resistant fungal species.
- Backes, Gregory L.,Jursic, Branko S.,Neumann, Donna M.
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p. 3397 - 3407
(2015/08/03)
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- Selectively catalytic epoxidation of α-pinene with dry air over the composite catalysts of Co-MOR(L) with Schiff-base ligands
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Twelve bi-/tridentate Schiff-base ligands (L1-L12) have been designed, synthesized and coordinated with ion-exchanged Co-MOR (Mordenite) forming a series of Co-MOR(L) composite catalysts, for which various analyzes and characterizations are conducted. Selectively catalytic epoxidation of α-pinene with dry air over Co-MOR(L) catalysts has been carried out, where uses TBHP in small amounts as the initiator. Among these Co-MOR(L) catalysts, Co-MOR(L8) exhibits the best activity for the titled reaction to obtain 85.8 mol% conversion and 90.8% selectivity of epoxide. Some factors such as the structure of ligands, the oxidants, the solvents, the catalyst amount, the reaction temperature and time play important roles in controlling the epoxidation. The recyclable stability of the Co-MOR(L8) catalyst is confirmed. The studies on the electrochemical behaviors of Co species in Co-MOR(L8) reveal the importance of reversible change between Co oxidation states for the epoxidation.
- Lu,Lei,Wei,Ma,Zhang,Hu,Zhou,Xia
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- Mononuclear and binuclear Cu(II) complexes of some tridentate aroyl hydrazones. X-ray crystal structures of a mononuclear and a binuclear complex
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Cu(II) complexes of eight N,N,O-donor hydrazone ligands, obtained by condensation of pyridine-2-carbaldehyde and 2-acetylpyridine with four aroyl hydrazides, are reported. Reactions of Cu(ClO4)2· 6H2O with the pyridine-2-c
- Mondal, Satyajit,Naskar, Sumita,Dey, Ayan Kumar,Sinn, Ekkehard,Eribal, Carla,Herron, Steven R.,Chattopadhyay, Shyamal Kumar
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