Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: Synthesis and in vitro biological evaluation. Part 1

Bozorov, Khurshed; Ma, Hao; Zhao, Jiaheng; Zhao, Haiqing; Chen, Hua; Бобакулов, Х. М.; Xin, Xuelei; Элмурадов, Б. Ж.; Shakhidoyatov, Khusnutdin M.; Aisa, Haji Akber

doi:10.1016/j.ejmech.2014.07.065

Cited by 30 publications

(19 citation statements)

References 33 publications

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“…The [3-(4,5-dimethylthiazolyl)-diphenyl tetrazolium bromide] (MTT) assay was performed using the method of Bozorov et al [33][34][35]. A stock solution of ethyl acetate extract of the fungus solution was prepared in 50 mg/mL DMSO.…”

Section: Cytotoxic Activity (Mtt Assay)mentioning

confidence: 99%

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: Cytotoxic Activity (Mtt Assay)mentioning

confidence: 99%

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

et al. 2020

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“…In addition, 2‐aminothiophene and its azomethine derivative 10 , synthesised from doubly activated nitriles as components in the Gewald reaction, have been screened in vitro for anticancer, antimicrobial, and antidiabetic activities against human breast, human cervical, and human endometrial cancer cell lines, as well as on Staphylococcus aureus , Escherichia coli (bacteria), and Candida albicans (fungi) types of microorganism .…”

Section: Gewald Reaction Modificationsmentioning

confidence: 99%

The Gewald reaction in dye chemistry

Sabnis¹

2016

Coloration Technology

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This review presents the most elegant and promising set of synthetic routes for the synthesis of 2‐aminothiophenes by the Gewald reaction. This reaction has applications in several applied fields, such as pharmaceuticals/biomedicine, agrochemicals, carbohydrate conjugates, sugar cane ripeners, peptide analogues, dyestuffs, and electronic materials; however, the present review will focus on the use of Gewald chemistry in the synthesis of conventional and functional colourants. The Gewald reaction produces 2‐aminothiophene, which is a key intermediate for the diazotisation reaction and for the synthesis of azo dyes, and thus opened the door for new dye chemistry. The reaction produces electron‐withdrawing groups such as CN, COOEt, COOMe, CONH2, and COPh in the 3‐ and/or 5‐position, resulting in bathochromic shifts for the deeper colours of the dyes. The review further reveals the importance of this reaction in the synthesis of azo dyes, fluorescent dyes (coumarin dyes, styryl dyes, thieno[2,3‐d]pyrimidine dyes, bithiophene dyes), thiophene analogues of phthalocyanines, and fluorescent whitening agents.

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“…Recently, we described Schiff bases of DDTD with only 4-substituents at the benzene ring (Chart 1) as potential anticancer and antimicrobial compounds and discussed the role of various substituents to DDTD under the aspect of structure activity relationships (SARs). 27 Among them, some promising nitroaromatic compounds were discovered which need further modications. On the other hand, although nitroaromatic drugs ( Fig.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and anti-influenza virus agents. Part 2

et al. 2017

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Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: Synthesis and in vitro biological evaluation. Part 1

Cited by 30 publications

References 33 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

The Gewald reaction in dye chemistry

Synthesis and in vitro biological evaluation of novel diaminothiophene scaffolds as antitumor and anti-influenza virus agents. Part 2

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