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Anti-Cancer Agents in Medicinal Chemistry

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ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

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Research Article

Synthesis and Evaluation of Cytotoxic Activity of Certain Benzo[h]chromene Derivatives

Author(s): Samir M. Awad, Mosaad S. Mohamed, Marwa Abd El-Fattah Khodair and Rania H. Abd El-Hameed*

Volume 21, Issue 8, 2021

Published on: 25 September, 2020

Page: [963 - 986] Pages: 24

DOI: 10.2174/1871520620666200925103742

Price: $65

Abstract

Background: Benzo[h]chromenes attracted great attention because of their widespread biological activities, including anti-proliferate activity, and the discovery of novel effective anti-cancer agents is imperative.

Objective: The main objective was to synthesize new benzo[h]chromene derivatives and some reported derivatives, and then test all of them for their anti-cancer activities.

Methods: The structures of the newly synthesized derivatives were confirmed by elemental and spectral analysis (IR, Mass, 1H-NMR and 13C-NMR). 35 compounds were selected by the National Cancer Institute (NCI) for single-dose testing against 60 cell lines and 3 active compounds were selected for 5-doses testing. Also, these 3 compounds were tested as EGFR-inhibitors; using sorafenib as standard, and as Tubulin polymerization inhibitors using colchicines as a standard drug. Moreover, molecular docking study for the most active derivative on these 2 enzymes was also carried out.

Results: Compounds 1a, 1c and 2b have the highest activities among all 35 tested compounds especially compound 1c.

Conclusion: compound 1c has promising anti-cancer activities compared to the used standards and may need further modification and investigations.

Keywords: Benzo[h]chromene, synthesis, anti-cancer activity, 5-doses testing, EGFR-inhibitors, tubulin polymerization inhibitors.

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