Title:Synthesis and Evaluation of Cytotoxic Activity of Certain Benzo[h]chromene Derivatives
VOLUME: 21 ISSUE: 8
Author(s):Samir M. Awad, Mosaad S. Mohamed, Marwa Abd El-Fattah Khodair and Rania H. Abd El-Hameed*
Affiliation:Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Helwan, Cairo, Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Helwan, Cairo, Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Helwan, Cairo, Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Helwan, Cairo
Keywords:Benzo[h]chromene, synthesis, anti-cancer activity, 5-doses testing, EGFR-inhibitors, tubulin polymerization inhibitors.
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.
