In Vitro and In Vivo Anti-Breast Cancer Activities of Some Newly Synthesized 5-(thiophen-2-yl)thieno-[2,3-d]pyrimidin-4-one Candidates

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2019 Jun 20

PMID 31212962

Citations 2

Authors

Abd El-Galil E Amr

Alhussein A Ibrahimd

Mohamed F El-Shehry

Hanaa M Hosni

Ahmed A Fayed

Elsayed A Elsayed

Affiliations

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Abstract

In this study, some of new thiophenyl thienopyrimidinone derivatives - were prepared and tested as anti-cancer agents by using thiophenyl thieno[2,3-d]pyrimidinone derivative as a starting material, which was prepared from cyclization of ethyl ester derivative with formamide. Treatment of with ethyl- chloroacetate gave thienopyrimidinone -ethylacetate , which was reacted with hydrazine hydrate or anthranilic acid to afford acetohydrazide and benzo[d][1,]oxazin-4-one respectively. Condensation of with aromatic aldehydes or phenylisothiocyanate yielded Schiff base derivatives , and thiosemicarbazise , which were treated with 2-mercaptoacetic acid or chloroacetic acid to give the corresponding thiazolidinones , and phenylimino-thiazolidinone , respectively. Treatment of with ethylacetoacetate or acetic acid/acetic anhydride gave pyrazole and acetyl acetohydrazide derivatives, respectively. The latter compound was reacted with ethyl cycno-acetate or malononitrile to give and , respectively. In this work, we have studied the anti-cancer activity of the synthesized thienopyrimidinone derivatives against MCF-7 and MCF-10A cancer cells. Furthermore, in vivo experiments showed that the synthesized compounds significantly reduced tumor growth up to the 8 day of treatment in comparison to control animal models. Additionally, the synthesized derivatives showed potential inhibitory effects against pim-1 kinase activities.

Citing Articles

In Vitro Cytotoxicity and In Vivo Antitumor Activity of Lipid Nanocapsules Loaded with Novel Pyridine Derivatives.

Lila A, Amran M, Tantawy M, Moglad E, Gad S, Alotaibi H Pharmaceutics. 2023; 15(6).

PMID: 37376202 PMC: 10304225. DOI: 10.3390/pharmaceutics15061755.

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules.

Elkaeed E, Abd El Salam H, Sabt A, Al-Ansary G, Eldehna W Molecules. 2021; 26(24).

PMID: 34946704 PMC: 8709016. DOI: 10.3390/molecules26247611.

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