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