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

Mai A Mansour; Mamdouh A Oraby; Zeinab A Muhammad; Deena S Lasheen; Hatem M Gaber; Khaled A M Abouzid

doi:10.1039/d2ra00889k

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

RSC Adv. 2022 Mar 15;12(13):8193-8201. doi: 10.1039/d2ra00889k. eCollection 2022 Mar 8.

Authors

Mai A Mansour¹, Mamdouh A Oraby², Zeinab A Muhammad³, Deena S Lasheen⁴, Hatem M Gaber³, Khaled A M Abouzid^{4

5}

Affiliations

¹ Pharmaceutical Chemistry Department, Faculty of Pharmacy, Badr University in Cairo Cairo Egypt maiali92@yahoo.com.
² Pharmacology Department, Faculty of Pharmacy, Badr University in Cairo Cairo Egypt.
³ National Organization for Drug Control and Research Cairo Egypt.
⁴ Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ain Shams University, Abbassia Cairo 11566 Egypt khaled.abouzid@pharma.asu.edu.eg.
⁵ Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City Menoufia Sadat City Egypt.

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.