title: Solvent free synthesis, anti-inflammatory and anticancer activity evaluation of tricyclic and tetracyclic benzimidazole derivatives.
abstract: 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 p.o. compounds 3b (39.4%) and 3c (39.2%) exhibited anti-inflammatory activity, comparable to standard ibuprofen which showed 39% activity at 50 mg/kg p.o. and compound 7c exhibit good anticancer activity against ovary (IGR-OV-1), breast (MCF-7) and CNS(SF-295) human cancer cell lines.
authors.affiliation: Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247 667 UK, India. sondifcy@iitr.ernet.in
authors.forename: Sham M
authors.initials: SM
authors.lastname: Sondhi
authors.forename: Reshma
authors.initials: R
authors.lastname: Rani
authors.forename: Jaiveer
authors.initials: J
authors.lastname: Singh
authors.forename: Partha
authors.initials: P
authors.lastname: Roy
authors.forename: S K
authors.initials: SK
authors.lastname: Agrawal
authors.forename: A K
authors.initials: AK
authors.lastname: Saxena
mesh_terms: D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005260:Female; D006801:Humans; D008872:Microwaves; D009369:Neoplasms / Q000188:drug therapy*; D010051:Ovarian Neoplasms / Q000188:drug therapy
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D001562:Benzimidazoles