Design, Synthesis and Anticancer Screening of Novel Pyrazole Derivatives Linking to Benzimidazole, Benzoxazole and Benzothiazole
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منابع مشابه
Design, Synthesis and Anticancer Screening of Novel Pyrazole Derivatives Linking to Benzimidazole, Benzoxazole and Benzothiazole
Substituted aromatic amines were diazotized followed by coupling with malononitrile to afford substituted phenyl hydrazono-malononitrile compounds 2a-c. Compounds 3a-c were prepared through the reaction of substituted phenyl hydrazono-malononitriles 2a-c with phenyl hydrazine, while the reaction of compounds 2a-c with hydrazine hydrate afforded diamino compounds 4a-c. The diamino compounds 4a-c...
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In this study an easy, green, efficient and simple approach is reported for the synthesis of some benzothiazole-, benzimidazole- and benzoxazole-2-thiolderivatives. The proposed approach employs the reaction of corresponding aromatic amine with potassium isopropyl xanthate (Z11) in the presence of copper sulfate (CuSO4) as a catalyst under conventional heating and ultrasonic irr...
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In a previous hit-to-lead research program targeting anticancer agents, two promising lead compounds, 1a and 1b, were found. However, the poor solubility of 1a and 1b made difficult further in vivo studies. To solve this problem, a lead optimization was conducted through introducing N-methyl-piperazine groups at the 2-position and 6-position. To our delight, the optimized analogue 1d showed com...
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The synthesis of (S)-2-(4-tert-butylphenoxy)-3-(benzoxazol-5-yl) propanoic acid derivatives (2a-k) were described and their in vitro antibacterial activities were determined against Gram-negative and -positive bacteria. These compounds were found to exert a broad spectrum of activity against the screened bacteria, but poor MIC values were found for Candida albicans fungi. Compound 2b bearing a ...
متن کاملSynthesis and antimicrobial activity of some novel 2,5- and/or 6-substituted benzoxazole and benzimidazole derivatives.
A new series of 2,5- and/or 6-substituted benzoxazoles (7a-f), benzimidazoles (8a-g) holding cyclohexyl or cyclopentyl moieties at position 2 and 5- or 6-substituted-2-cyclohexylaminomethylbenzoxazoles (9a, b) was synthesized in order to determine their antimicrobial activities and feasible structure-activity relationships. The synthesized compounds were tested in vitro against three Gram-posit...
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ژورنال
عنوان ژورنال: Medicinal Chemistry
سال: 2014
ISSN: 2161-0444
DOI: 10.4172/2161-0444.s1-001