Nicotinamide-based diamides derivatives as potential cytotoxic agents: synthesis and biological evaluation

Peng, Min; Shi, Liqiao; Ke, Shaoyong

doi:10.1186/s13065-017-0338-5

Cited by 14 publications

(8 citation statements)

References 23 publications

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“…Due to the appreciable stability with time of the complex in DMSO under physiological-like conditions, the complex could be evaluated as potential cytotoxic agent. Previously, many studies were reported the cytotoxicity properties of NA [67][68][69][70]. Hence, the cytotoxicity of the BBHMP and its platinum(II) complex was examined for human prostate (DU145) and breast (MCF7) cancer cell lines with an MTT assay.…”

Section: Cytotoxicity Resultsmentioning

confidence: 99%

Synthesis and Biological Activity of a New Pt(II) Complex Involving 4-bromo-2,6-bis-hydroxymethyl-phenol and Nicotinamide

Altun

Yoruç

Boz

2021

Preprint

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In the presented study, Pt(II) complex including 4-Bromo-2,6-bis-hydroxymethyl-phenol (BBHMP) and nicotinamide (NA) was synthesized and structurally analyzed by using spectral and thermal analysis methods. The BBHMP and its Pt(II) complex involving BBHMP and NA were investigated for their antimicrobial, cytotoxicity, gen expression and antioxidant properties. The antimicrobial activity results showed that the platinum complex displayed moderate antibacterial and antifungal activities. The cytotoxicity of the BBHMP and platinum complex were determined against human prostate (DU145) and breast (MCF7) cancer cell lines by applying MTT assay. Cytotoxicity results suggest that the Pt(II) complex exhibited moderate cytotoxicity against growth of used cancer cell lines when compared with the reference drug cisplatin. Gen expression results proved that Pt(II) complex is a special bioactive chemical constituent and potential anticancer agent. In addition, the complex demonstrated important antioxidant activity.

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Section: Cytotoxicity Resultsmentioning

confidence: 99%

Synthesis and Biological Activity of a New Pt(II) Complex Involving 4-bromo-2,6-bis-hydroxymethyl-phenol and Nicotinamide

Altun

Yoruç

Boz

2021

Preprint

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“…Amide protons were identified between 8.7 ppm and 8.3 ppm in all compounds. 16 Similarly triplet and doublet protons of compound 3 vanished in compound 4. This absent confirmed the ester hydrolyzed product (4).…”

Section: Preparation Of N-substituted-2-(nicotinamido) Thiazole-4-carboxamide (5a-i)mentioning

confidence: 94%

Synthesis, Characterisation and Antimicrobial Activity of New Nicotinamide-Thiazole Derivatives

Venkatasubramanian¹,

Sha²,

Hemalatha³

et al. 2019

RJC

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In this era, the identification or synthesis of a new antibiotic is important research due to the pollution and harmful bacterial pathogens. Hence this work selected the already known mild active molecules such as Nicotinamide and Thiazole to enhance the activity against the disease-causing pathogens. Using peptide coupling reagent EDCI, nine compounds were prepared and characterized by 1 H NMR, Mass spectroscopy. The characterized compounds were evaluated In vitro antibacterial and antifungal activity against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumonia, Candida albicans by broth dilution method and zone of inhibition measured in millimeter. All the derivatives showed good to moderate activity. Out of nine compounds N- (4-(thiomorpholine-4-carbonyl) thiazol-2-yl) nicotinamide showed better zone of inhibition between 27 mm and 34 mm. the outcomes of the result revealed that the diamide bond acts as an important pharmacophore and exposed the good inhibition behavior.

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“…Recently, during the course of our research on discovery of functional molecules, a series of diamides derivatives bearing nicotinamide unit were obtained ( Peng et al, 2017 ), and an interesting phenomenon was found based on the preliminary results. All of the similar diamides without nicotinamide moiety lost the inhibitory activity except the compound bearing diarylamine unit ( A2 , R = Me), and this compound exhibited good cytotoxic activity against the tested lung cancer cell lines (NCI-H460, A549, and NCI-H1975) with IC 50 values of 14.66–46.42 μM ( Figure 2 ).…”

Section: Introductionmentioning

confidence: 99%

Diarylamine-Guided Carboxamide Derivatives: Synthesis, Biological Evaluation, and Potential Mechanism of Action

Huang

Zhang

et al. 2022

Front. Chem.

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Diarylamines are a class of important skeleton widely existing in drugs or natural products. To discover novel diarylamine analogues as potential drugs, two series of diamide and carboxamide derivatives containing diarylamine scaffold were designed, synthesized and evaluated for their potential cytotoxic activities. The bioassay results indicated that some of the obtained compounds (C5, C6, C7, C11) exhibited good cytotoxic effect on cancer cell lines (SGC-7901, A875, HepG2), especially, compound C11 present significantly selective proliferation inhibition activity on cancer and normal cell lines (MARC145). In addition, the possible apoptosis induction for highly potential molecules was investigated, which present compound C11 could be used as novel lead compound for discovery of promising anticancer agents.

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Nicotinamide-based diamides derivatives as potential cytotoxic agents: synthesis and biological evaluation

Cited by 14 publications

References 23 publications

Synthesis and Biological Activity of a New Pt(II) Complex Involving 4-bromo-2,6-bis-hydroxymethyl-phenol and Nicotinamide

Synthesis and Biological Activity of a New Pt(II) Complex Involving 4-bromo-2,6-bis-hydroxymethyl-phenol and Nicotinamide

Synthesis, Characterisation and Antimicrobial Activity of New Nicotinamide-Thiazole Derivatives

Diarylamine-Guided Carboxamide Derivatives: Synthesis, Biological Evaluation, and Potential Mechanism of Action

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