Synthesis and anticancer evaluation of bis furfurylidene-4-piperidone analog of 5-fluorouracil

Abstract

5-Fluorouracil (5-FU) displayed several side effects due to its nonspecific cytotoxicity for tumour cells. In order to overcome these disadvantages, numerous modifications of the 5-fluorouracil structure have been performed. In the present study, bis furfurylidene-4-piperidone substituted 5-flurouracil derivative is prepared and evaluated against various cancer cells. The resultant derivative is characterized by spectral data. This compound having 1,5-diaryl-3-oxo-1,4-pentadinenyl pharmacophore which interact with cellular thiols and produces cytotoxic activity whereas 5-flurouracil part showed anticancer activity by interacting with nucleic acid. The resulting synthesized compound has been screened for in vitro cytotoxic property by SRB assay method against breast and colon cancer cell lines. The results indicate that, this compound showed equipotent cytotoxicity against human breast cell lines as compared to standard, 5-flurouracil and doxorubicin. Acute toxicity was determined by OECD-423 guidelines. In vivo anticancer activity was evaluated in Swiss albino mice bearing Ehrlich Ascites Carcinoma (EAC). This compound showed significant anticancer activity against Ehrlich Ascites Carcinoma in Swiss albino mice. This study revealed the potentiality of this molecule for further development as anticancer agents.