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  • Chem Sci Trans., 2012, 1(3),  pp 624-631  

    DOI:10.7598/cst2012.272

    Research Article

    Synthesis, In Vitro Evaluation of Some Novel Quinazolin-4(3H)-one Derivatives as Anti-Tumor Agents

  • K. SRIVALLI* and K. SATISH
  • Department of Pharmaceutical Chemistry, Bharat Institute of Technology (Pharmacy), Ibrahimpatnam, Hyderabad, Andhra Pradesh, India
  • Abstract

    In an effort to develop anticancer agents, a series of Mannich bases were prepared by Mannich reaction. When one biologically active molecule is linked to another, the resultant molecule generally has increased potency. Hence two pharmacophores, i.e. quinazoline ring and amine moiety are fused to obtain highly potent, more specific and less toxic agent. In the present study, synthesis of novel quinazolin-4(3H)-one derivatives by condensation of appropriate quinazolines with various p-substituted primary amines in presence of glacial acetic acid and ethanol at room temperature (Mannich reaction). Synthesized compounds were characterized; both analytical and spectral data (UV, IR, GC-MS, 1H NMR) of all derivatives were in full agreement with proposed structures. All the derivatives were tested for their anti-tumor activity by two in vitro studies like Brine shrimp Lethality assay and Trypan blue exclusion assay.

    Keywords

    Quinazolinones, Mannich reaction, Brine shrimp lethality assay, Trypan blue exclusion assay

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