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 |
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Format: | Artikel |
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2010.01.147 |