Identification of novel furo[2,3-d]pyrimidine based chalcones as potent anti-breast cancer agents: synthesis, in vitro and in vivo biological evaluation
Mansour, Mai A; Oraby, Mamdouh A; Muhammad, Zeinab A; Lasheen, Deena; Gaber, Hatem M; Khaled A M Abouzid;
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.
Other data
Title | Identification of novel furo[2,3-d]pyrimidine based chalcones as potent anti-breast cancer agents: synthesis, in vitro and in vivo biological evaluation | Authors | Mansour, Mai A; Oraby, Mamdouh A; Muhammad, Zeinab A; Lasheen, Deena ; Gaber, Hatem M; Khaled A M Abouzid | Keywords | HYBRIDS;ANTICANCER ACTIVITY;MOLECULAR TARGETS;CYTOTOXICITY;DERIVATIVES;APOPTOSIS | Issue Date | 8-Mar-2022 | Publisher | ROYAL SOC CHEMISTRY | Journal | RSC Advances | Volume | 12 | Issue | 13 | Start page | 8193 | End page | 8201 | DOI | 10.1039/d2ra00889k | PubMed ID | 35424720 | Scopus ID | 2-s2.0-85127335669 | Web of science ID | WOS:000769025000001 |
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