Solvent free synthesis, anti-inflammatory and anticancer activity evaluation of tricyclic and tetracyclic benzimidazole derivatives

Heterocyclic benzimidazole derivatives 3a–h, 5a-c and 7a–d have been synthesized by via microwave irradiation in good yields and their evaluation for anti-inflammatory and anticancer activity is reported. Heterocyclic benzimidazole derivatives 3a– h, 5a– c and 7a– d have been synthesized by condensa...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2306-2310
Hauptverfasser: Sondhi, Sham M., Rani, Reshma, Singh, Jaiveer, Roy, Partha, Agrawal, S.K., Saxena, A.K.
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Sprache:eng
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Zusammenfassung:Heterocyclic benzimidazole derivatives 3a–h, 5a-c and 7a–d have been synthesized by via microwave irradiation in good yields and their evaluation for anti-inflammatory and anticancer activity is reported. Heterocyclic benzimidazole derivatives 3a– h, 5a– c and 7a– d have been synthesized by condensation of succinic acid ( 1) homophthalic acid ( 4) and 2,3-pyrazinedicarboxlic acid ( 6) with various substituted diamines under microwave irradiation in good yields. Structures assigned to 3a– h, 5a– c and 7a– d are fully supported by spectral data. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50 mg/kg po compounds 3b (39.4%) and 3c (39.2%) exhibited anti-inflammatory activity, comparable to standard ibuprofen which showed 39% activity at 50 mg/kg po and compound 7c exhibit good anticancer activity against ovary (IGR-OV-1), breast (MCF-7) and CNS(SF-295) human cancer cell lines.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.147