Identification of novel furo[2,3-d]pyrimidine based chalcones as potent anti-breast cancer agents: synthesis, in vitro and in vivo biological evaluation

Various substituted synthetic chalcones demonstrated potent anti-cancer activities. In the current study a series of novel furo[2,3-d]pyrimidine based chalcones were synthesized as potential anticancer agents. Among the different substituted derivatives, two of the halogen bearing chalcones, 5d and 5e, demonstrated potent anti-proliferative activity against an NCI 59 cell line, with mean GI(50) values of 2.41 mu M and 1.23 mu M, respectively. Moreover, both compounds showed pronounced cytotoxic activity (5d; 1.20 +/- 0.21, 5e; 1.90 +/- 0.32) against the resistant MCF-7 cell line when compared to doxorubicin; 3.30 +/- 0.18. Such outcomes provoked the initiation of an in vivo anticancer assessment study, where compound 5e revealed comparable results to doxorubicin.

Automated summary

Synthetic furo[2,3-d]pyrimidine-based chalcones exhibited potent anti-proliferative and cytotoxic activities against cancer cells. Among the halogen-bearing derivatives, compounds 5d and 5e showed significant anti-proliferative activity against a resistant cell line and comparable efficacy to doxorubicin in in vivo anticancer assessment.