Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells

Nie, Li; Bozorov, Khurshed; Niu, Chao; Huang, Guozheng; Aisa, Haji Akber

doi:10.1007/s11164-017-3023-3

Cited by 17 publications

(6 citation statements)

References 23 publications

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“…The melanin content was determined in accordance with the procedure described previously [27][28][29][30]. B16 cells were seeded in a six-well plate at a concentration of 2 × 10 5 cells per well and incubated for 24 h. The cultured B16 cells were further incubated in the absence or the presence of the sample for 48 h. Each well with cells was then washed twice with ice-cold PBS.…”

Section: Melanin Measurementmentioning

confidence: 99%

“…B16 cells were seeded in a six-well plate at a concentration of 2 × 10 5 cells per well and incubated for 24 h. The cultured B16 cells were further incubated in the absence or the presence of the sample for 48 h. Each well with cells was then washed twice with ice-cold PBS. Cells were then lysed as described previously [28]. A total of 150 µL aliquots of each lysate were put in a 96-well microplate and absorbance was read spectrophotometrically at 405 nm using a multi-plate reader.…”

Section: Melanin Measurementmentioning

confidence: 99%

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Biological Activity of Endophytic Fungi from the Roots of the Medicinal Plant Vernonia anthelmintica

et al. 2020

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Endophytic fungi were first isolated from the fresh root of the Chinese medicinal plant Vernonia anthelmintica collected from the Hotan Prefecture within the Xinjiang Autonomous region of the People’s Republic of China. This plant has been used in Uyghur traditional medicine to treat vitiligo, a skin condition characterized by patches of the skin losing their pigment. In total, fifteen fungal strains were isolated. Among these, four endophytic fungi were identified by their DNA sequences and registered to GenBank with accession numbers. The isolates were identified as Schizophyllum commune XJA1, Talaromyces sp. XJA4, Aspergillus sp. XJA6, Aspergillus terreus XJA8. Ethyl acetate extracts of all fungal strains were used to quantify melanin content and to identify in vitro biological activity assays including antimicrobial, antioxidant, cytotoxic, antidiabetic and tyrosinase activity on B16 cells. Among the extracts of all four identified strains, the ethyl acetate extract of the Aspergillus sp. XJA6 was chosen for further characterization because it presented the highest biological activity against these tests. In addition, twenty four volatile compounds from the petroleum ether fraction were characterized by GC–MS.

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Section: Melanin Measurementmentioning

confidence: 99%

Section: Melanin Measurementmentioning

confidence: 99%

Biological Activity of Endophytic Fungi from the Roots of the Medicinal Plant Vernonia anthelmintica

et al. 2020

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“…After the addition was complete, the thick mass was heated for 8 h at 130 ο C, then cooled and washed with methanol. The crude product was dissolved in hot water and the aminothiazole was precipitated by the addition of NH 4…”

Section: N-(4-(2-aminothiazol-4-yl)phenyl) Benzenesulfonamide (4)mentioning

confidence: 99%

“…Aryl/heteroaryl sulfonamides are versatile compounds of significant synthetic and biological properties that are widely applied . The synthesis of various sulfonamide derivatives has attracted substantial interest as many of them show wonderful anticancer activity in vitro and in vivo against diverse cancer cell lines .…”

Section: Introductionmentioning

confidence: 99%

“…Aryl/heteroaryl sulfonamides are versatile compounds of significant synthetic and biological properties that are widely applied. [1][2][3][4] The synthesis of various sulfonamide derivatives has attracted substantial interest as many of them show wonderful anticancer activity in vitro and in vivo against diverse cancer cell lines. [5][6][7] There are a number of mechanisms that illustrate the anticancer action of sulfonamides, including carbonic anhydrase inhibition, disruption of microtubule assembly, cell cycle release in the G1 phase, functional suppression of the transcriptional activator NF-Y, and inhibition of angiogenesis among others.…”

Section: Introductionmentioning

confidence: 99%

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Convenient synthesis of novel sulfonamide derivatives as promising anticancer agents

El‐Mekabaty

Awad

2019

Journal of Heterocyclic Chem

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Novel sulfonamide derivatives have been synthesized from the readily accessible N‐(4‐acetylphenyl)benzenesulfonamide (1). Condensation of 1 with phenylhydrazine in refluxing ethyl alcohol gave the corresponding phenylhydrazone 2, which was then added to the Vilsmeier‐Haack reagent (POCl3/DMF) to give the 4‐formylpyrazole derivative 3. Fusion of 1 with thiourea in the presence of iodine at 130°C afforded the 2‐aminothiazole derivative 4. Refluxing 1 with an excess of N, N‐dimethylformamide dimethyl acetal furnished the enaminone 5. The chemical reactivity of enaminone 5 toward some nitrogen and carbon nucleophiles has been studied to obtain polyfunctionalized heteroaromatic systems bearing a sulfonamide moiety. Besides, the enaminone 5 undergoes the Gewald reaction and reacts with ethyl cyanoacetate and elemental sulfur in the presence of morpholine to yield the 2‐aminothiophene derivative 18. Moreover, the utility of 5 for the synthesis of 4‐(phenylsulfonamido)benzoic acid (19) was investigated. The synthesized sulfonamides were evaluated for their in vitro cytotoxic activities against two human cell lines, MCF‐7 (breast adenocarcinoma cells) and RPE‐1 (normal retina pigmented epithelium cells). The results revealed that compounds 1‐3, 6‐8, 10, 12b, 18, 19, and 21 have a potent cytotoxic effect on MCF‐7 and less on RPE‐1 cells compared to the positive control doxorubicin®.

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Recent Developments on the Synthesis and Biological Activities of Fused Pyrimidinone Derivatives

2021

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Heterocyclic compounds constitute a unique class of organic compounds endowed with a wide range of synthetic and pharmaceutical applications. Pyrimidinones and their fused analogues have received focused attention in this regard, partly due to their mimicry of nucleobases which consequently forges their interesting medicinal properties. Over the years, the medicinal chemistry research community has experienced an upsurge in articles describing the exploration of these scaffolds to develop effective therapeutic agents. Several biological activities, including antimicrobial, antiviral, anticancer, antidiabetic, anti‐inflammatory, anticonvulsive, and antihistaminic, have been well documented. This minireview presents a compendium of recent developments (2017–2020) focused on the synthesis and biological activities of fused pyrimidinones. The goal is to update medicinal chemists on the therapeutic relevance of fused pyrimidinones and the molecular architecture of clinic‐worthy drug candidates. A brief account of the structure‐activity relationships (SAR) revealed from different biological assays is also discussed.

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Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells

Cited by 17 publications

References 23 publications

Biological Activity of Endophytic Fungi from the Roots of the Medicinal Plant Vernonia anthelmintica

Biological Activity of Endophytic Fungi from the Roots of the Medicinal Plant Vernonia anthelmintica

Convenient synthesis of novel sulfonamide derivatives as promising anticancer agents

Recent Developments on the Synthesis and Biological Activities of Fused Pyrimidinone Derivatives

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