Dihydrithieno[2,3-b]naphto-4,9-dione analogues as anticancer agents: Synthesis and in cell pharmacological studies

Bertamino, Alessia; Musella, Simona; Sarno, Veronica Di; Ostacolo, Carmine; Manfra, Michele; Vanacore, Daniela; Stiuso, Paola; Novellino, Ettore; Campiglia, Pietro; Gómez-Monterrey, Isabel

doi:10.1016/j.ejmech.2015.07.044

Cited by 11 publications

(4 citation statements)

References 36 publications

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“…Lately, much interest has been focused on the chemistry and the biological activity of fused heterocyclic systems because of their broad spectrum of physiological activities [1,2]. Among these heterocyclic compounds carrying nitrogen atom, imidazo [2,1-b]thiazole derivatives possess specific importance because of their diverse pharmacological activities.…”

Section: Introductionmentioning

confidence: 99%

Design and synthesis of novel Imidazo[2,1-b]thiazole derivatives as potent antiviral and antimycobacterial agents

Gürsoy

Dincel

Naesens

et al. 2020

Bioorganic Chemistry

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A B S T R A C TA series of novel acyl-hydrazone (4a-d) and spirothiazolidinone (5a-d, 6a-d) derivatives of imidazo[2,1-b] thiazole were synthesized and evaluated for their antiviral and antimycobacterial activity. The antituberculosis activity was evaluated by using the Microplate Alamar Blue Assay and the antiviral activity was evaluated against diverse viruses in mammalian cell cultures. According to the biological activity studies of the compounds, 5a-c displayed hope promising antitubercular activity, 6d was found as potent for Coxsackie B4 virus, 5d was found as effective against Feline corona and Feline herpes viruses. Consequently, the obtained results displayed that, 5a-d and 6d present a leading structure for future drug development due to its straightforward synthesis and relevant bioactivity.

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Section: Introductionmentioning

confidence: 99%

Design and synthesis of novel Imidazo[2,1-b]thiazole derivatives as potent antiviral and antimycobacterial agents

Gürsoy

Dincel

Naesens

et al. 2020

Bioorganic Chemistry

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“…LPO has a serious role in triggering many pathological disorders by degrading cellular membrane integrity and leakage of cytoplasmic components. Free radical scavenging is a common system that inhibits lipid peroxidation in the body by antioxidants 50 . The TBARS assay is the most widely used method for determining the lipid peroxidation process.…”

Section: Resultsmentioning

confidence: 99%

Green synthesis of nanosized N,N'-bis(1-naphthylidene)-4,4'-diaminodiphenylmethane and its metal (II) complexes and evaluation of their biological activity

Hassan

Hussien

Elhusseiny

2022

Sci Rep

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Condensation of ecofriendly synthesized 4,4’-methanedianiline with 2-hydroxy-1-naphthaldehyde produced a (1:1) octopus-like Schiff base mixed ligand. Reaction with Co(OAc)2⋅H2O, NiCl2⋅6H2O, Cu(OAc)2⋅H2O and Zn(OAc)2⋅2H2O metals furnished their complexes in high yield and purity. All new structures were fully characterized by various spectroscopic and spectrometric measurements. The complexes exhibited high thermal stability up to 700 °C, leaving nearly 40% of their mass as residues. Antimicrobial screening results exhibited moderate activities towards all studied microbes. Antioxidant screening was concentration dependent, and their activities were in the order Ni(II) > Zn(II) > Cu(II) > Co(II) complexes. The NO inhibitory effect revealed that the nickel complex exhibited the highest activity, whereas the cobalt complex showed the lowest inhibition. All compounds showed a significant lipid peroxidation inhibitory effect against oxidative stress. The complexes significantly diminished the TBARS level, and the nickel complex exhibited the highest inhibition at p < 0.01. Antioxidants stress the oxidative damage induced by iron, indicating that the nickel complex has the highest reducing activity. The inhibitory effect against acetylcholine esterase showed that the copper complex has the highest activity. Membrane stabilization activities clearly indicated that most compounds can improve the integrity of the cells and stability of their membrane, and this result may be related to their antioxidant capacity to protect against cytotoxicity. The nickel complex exhibited a stronger total antioxidant capacity than the other complexes. The biological and antioxidant capacities of these complexes may make them promising candidates in pharmaceutical applications.

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“…LPO has a serious role in triggering many pathological disorders by degrading cellular membrane integrity and leakage of cytoplasmic components. Free radical scavenging is a common system that inhibits lipid peroxidation in the body by antioxidants [37]. The TBARS assay is the most widely used method for determining the lipid peroxidation process.…”

Section: Dpph Radical Scavenging Activitymentioning

confidence: 99%

Green synthesis of nanosized N,N'-bis(1-naphthylidene)-4,4'-diaminodiphenylmethane and its metal (II) complexes: Reaction mechanism and biological activity evaluation

Hassan

Hussien

Elhusseiny

2022

Preprint

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Clgondensation of ecofriendly synthesized 4,4’-methanedianiline with 2-hydroxy-1-naphthaldehyde produced a (1:1) octopus-like Schiff base mixed ligand. Reaction with Co(OAc)2. H2O, NiCl2.6H2O, Cu(OAc)2. H2O and Zn(OAc)2.2H2O metals furnished their complexes in high yield and purity. All new structures were fully characterized by various spectroscopic and spectrometric measurements. The complexes exhibited high thermal stability up to 700 °C, leaving nearly 4 % of their mass as residues. Antimicrobial screening results exhibited moderate activities towards all studied microbes. Antioxidant screening was concentration dependent, and their activities were in the order Ni(II) > Zn(II) > Cu(II) > Co(II) complexes. The NO inhibitory effect revealed that the nickel complex exhibited the highest activity, whereas the cobalt complex showed the lowest inhibition. All compounds showed a significant lipid peroxidation inhibitory effect against oxidative stress. The complexes significantly diminished the TBARS level, and the nickel complex exhibited the highest inhibition at p < 0.01. Antioxidants stress the oxidative damage induced by iron, indicating that the nickel complex has the highest reducing activity. The inhibitory effect against acetylcholine esterase showed that the copper complex has the highest activity. Membrane stabilization activities clearly indicated that most compounds can improve the integrity of the cells and stability of their membrane, and this result may be related to their antioxidant capacity to protect against cytotoxicity. The nickel complex exhibited a stronger total antioxidant capacity than the other complexes. The biological and antioxidant capacities of these complexes may make them promising candidates in pharmaceutical applications.

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Dihydrithieno[2,3-b]naphto-4,9-dione analogues as anticancer agents: Synthesis and in cell pharmacological studies

Cited by 11 publications

References 36 publications

Design and synthesis of novel Imidazo[2,1-b]thiazole derivatives as potent antiviral and antimycobacterial agents

Design and synthesis of novel Imidazo[2,1-b]thiazole derivatives as potent antiviral and antimycobacterial agents

Green synthesis of nanosized N,N'-bis(1-naphthylidene)-4,4'-diaminodiphenylmethane and its metal (II) complexes and evaluation of their biological activity

Green synthesis of nanosized N,N'-bis(1-naphthylidene)-4,4'-diaminodiphenylmethane and its metal (II) complexes: Reaction mechanism and biological activity evaluation

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