Synthesis and electrochemical, spectral, and biological evaluation of novel 9,10-anthraquinone derivatives containing piperidine unit as potent antiproliferative agents

Niedziałkowski, Paweł; Czaczyk, Elżbieta; Jarosz, Jerzy; Wcisło, Anna; Białobrzeska, Wioleta; Wietrzyk, Joanna; Ossowski, Tadeusz

doi:10.1016/j.molstruc.2018.07.070

Cited by 15 publications

(8 citation statements)

References 52 publications

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“…[27,28] In addition to these heterocyclic aromatic compounds, aliphatic heterocyclic compounds such as morpholine, piperidine, and pyrrolidine are other examples of bioactive compounds used in many fields and pharmaceutical chemistry in particular. [29][30][31][32][33] In light of the significant literature data mentioned above, the main purpose of this study is to synthesize 2,6-disubstituted and 2,5,6-trisubstituted imidazo [2,1-b] [1,3,4]thiadiazole derivatives, to characterize these compounds using various spectroscopic methods, and to investigate their antimicrobial activity.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, Characterization, Antimicrobial Evaluation, and Computational Investigation of Substituted Imidazo[2,1‐b][1,3,4]Thiadiazole Derivatives

Dagli

Karakurt

et al. 2020

ChemistrySelect

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In this study, a novel series of 2,6-disubstituted and 2,5,6trisubstituted imidazo[2,1-b][1,3,4]thiadiazole derivatives were synthesized starting from 2-amino-1,3,4-thiadiazole derivatives. Structures of the synthesized compounds were characterized using various analysis techniques. Then, in vitro biological activity tests were carried out for all synthesized compounds and they were found to show moderate to good activity against all bacteria and fungi tested. Next, molecular docking simulations were performed to observe the inhibition effect of the synthesized compounds on the 3R9C receptor and support their biological activity results. Finally, the pharmacokinetic, ADME and toxicity properties of all compounds were examined using FAF-Drugs and ProTox webservers and it was concluded that they had acceptable toxicity and ADME properties.

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Section: Introductionmentioning

confidence: 99%

“…In addition to these heterocyclic aromatic compounds, aliphatic heterocyclic compounds such as morpholine, piperidine, and pyrrolidine are other examples of bioactive compounds used in many fields and pharmaceutical chemistry in particular …”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization, Antimicrobial Evaluation, and Computational Investigation of Substituted Imidazo[2,1‐b][1,3,4]Thiadiazole Derivatives

Dagli

Karakurt

et al. 2020

ChemistrySelect

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“…were evaluated for in vitro anti‐proliferative activity against the human cancer cell lines: HL‐60, LoVo, HL‐60/MX2, and LoVo/Dx. Compound 82 was most active against colon cancer cell lines and had 5–8 times higher activity against normal fibroblasts cell lines [129] . Xin‐Hua et al .…”

Section: Anti‐cancer Agentsmentioning

confidence: 99%

“…Compound 82 was most active against colon cancer cell lines and had 5-8 times higher activity against normal fibroblasts cell lines. [129] Xin-Hua et al synthesized various piperidine-bearing pyrazole hybrids and evaluated their anti-cancer potential against SGC-7901, MGC-803, and Bcap-37 cell lines. Compounds 83 a-b showed the most potent inhibitory activity, with an IC 50 value of 2.00 μM.…”

Section: Anti-cancer Agentsmentioning

confidence: 99%

Versatile Therapeutic Values of N‐Containing Heterocycles Benzimidazole, Piperazine and Piperidine Hybrids

Zala,

Kumari

2023

ChemistrySelect

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Nitrogen‐containing benzimidazole, piperazine, and piperidine are significant pharmacophores in medicinal chemistry and drug development. Many medications, lead compounds, and various reagents have these N‐containing scaffolds. This review concentrated on the development of novel therapeutic agents as well as the broad range of pharmacological actions demonstrated by benzimidazole, piperazine, and piperidine hybrids. The review emphasizes these hybrids′ potential, range, and medical significance. The review also discusses the structural criteria for benzimidazole, piperazine, and piperidine hybrids created by diverse chemists to be physiologically effective against a variety of disorders.

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“…The risk of developing cardiotoxicity against the background of treating carcinogenic pathologies is one of the most urgent problems of modern oncology and cardiology. Piperidine derivatives are of exceptional interest due to their potential biological activity, such as antiviral, antibacterial, antitumor, and many others [ 1 ].…”

Section: Introductionmentioning

confidence: 99%

Using the Correlation Intensity Index to Build a Model of Cardiotoxicity of Piperidine Derivatives

Toropova,

Toropov,

Roncaglioni

et al. 2023

Molecules

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The assessment of cardiotoxicity is a persistent problem in medicinal chemistry. Quantitative structure–activity relationships (QSAR) are one possible way to build up models for cardiotoxicity. Here, we describe the results obtained with the Monte Carlo technique to develop hybrid optimal descriptors correlated with cardiotoxicity. The predictive potential of the cardiotoxicity models (pIC50, Ki in nM) of piperidine derivatives obtained using this approach provided quite good determination coefficients for the external validation set, in the range of 0.90–0.94. The results were best when applying the so-called correlation intensity index, which improves the predictive potential of a model.

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Synthesis and electrochemical, spectral, and biological evaluation of novel 9,10-anthraquinone derivatives containing piperidine unit as potent antiproliferative agents

Cited by 15 publications

References 52 publications

Synthesis, Characterization, Antimicrobial Evaluation, and Computational Investigation of Substituted Imidazo[2,1‐b][1,3,4]Thiadiazole Derivatives

Synthesis, Characterization, Antimicrobial Evaluation, and Computational Investigation of Substituted Imidazo[2,1‐b][1,3,4]Thiadiazole Derivatives

Versatile Therapeutic Values of N‐Containing Heterocycles Benzimidazole, Piperazine and Piperidine Hybrids

Using the Correlation Intensity Index to Build a Model of Cardiotoxicity of Piperidine Derivatives

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