Synthesis and anticancer activity of some novel 3-(1, 3, 4-thiadiazol-2-yl)-quinazolin-4-(3H)-ones

• Autor(a) principal: Joseph, Alex
• Data de Publicação: 2010
• Outros Autores: Pai, Aravinda, Srinivasan, K. K., Kedar, Tukaram, Thomas, Angel Treasa, E. M., Jessy, Singla, Rajeev K.
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UFMS
• Texto Completo: https://repositorio.ufms.br/handle/123456789/5322
• topic: CNPQ::CIENCIAS EXATAS E DA TERRA::QUIMICA; Ascite; Carcinoma; Neoplasias; Quinazolinonas; Colorimetria; Técnicas de Química Analítica; HeLa; Linhagem Celular; Antineoplásicos; Ascites; Neoplasms; Quinazolinones; Colorimetry; Chemistry Techniques, Analytical; Cell Line; Antineoplastic Agents

Quinazolinone is a versatile lead molecule for designing potential bioactive agents. The compounds that have quinazolin-4-ones moiety are associated with interesting biological activities such as antifungal, antibacterial, antiviral, antitubercular and anticancer. In view of this we have undertaken synthesis of various thiadiazol substituted quinazolin-4-(3H)-ones. Novel 3-(1, 3, 4-thiadiazol-2-yl)-quinazolin-4-(3H)-ones (5a-5h) were synthesized by reaction of 5-alkyl/aryl substituted 1, 3, 4-thiadiazoles with 2-methyl/phenyl-4H-1, 3-benzooxazin-4-ones in the presence of pyridine. All the synthesized compounds were characterized by spectral and physical data. In vitro anticancer activity of all the synthesized compounds was determined by MTT assay on HeLa (Human cervical cancer cell) cells. Most active compounds found in vitro studies were further evaluated for their in vivo activity on Liquid tumor (Ehrlich’s Ascites Carcinoma; EAC) induced mice. The anticancer activity of compound 5f was found to be comparable to that of cisplatin against HeLa cells and was also effective in preventing the growth of tumor in mice as indicated by decrease in progressive gain in body weight as well as increase in life span when compared to animals of control group.