Abstract
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 GI50 values of 2.41 μM and 1.23 μM, 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.
Highlights
Discovery of a novel anticancer agent with reasonable potency, minor side effects and combating drug resistance has been a continuous vital need in the treatment of the various types of cancer
Synthesis of the designed furo[2,3-d]pyrimidine based chalcones started by reacting the active acetyl acetone (1) with sulfuryl chloride to afford the a-chloro acetylacetone (2) as mentioned earlier by Roland Verhie in 1978.20 The preparation of the furan derivative (3) was achieved by reacting (2) with malononitrile in a solution of sodium ethoxide according to the reported method.[21]
All the compounds were selected by the National Cancer Institute (NCI), USA for in vitro anti-cancer screening
Summary
Discovery of a novel anticancer agent with reasonable potency, minor side effects and combating drug resistance has been a continuous vital need in the treatment of the various types of cancer. Volume, following intraperitoneal administration of two different doses (2.5 & 5 mg per kg per day) of both tested compounds (5e & 5d) depicted a signi cant decrease in the tumor volume measured at day 5, 10, 15, and 20 versus the corresponding untreated EAT mice.
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