Identification of novel furo[2,3-]pyrimidine based chalcones as potent anti-breast cancer agents: synthesis, and 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 an...

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Published in:RSC advances 2022-03, Vol.12 (13), p.8193-821
Main Authors: Mansour, Mai A, Oraby, Mamdouh A, Muhammad, Zeinab A, Lasheen, Deena S, Gaber, Hatem M, Abouzid, Khaled A. M
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Summary: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 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. Various substituted synthetic chalcones demonstrated potent anti-cancer activities.
ISSN:2046-2069
DOI:10.1039/d2ra00889k