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

Background: Benzo[h]chromenes attracted great attention because of their widespread biological activities including antiproliferate activity, and the discovery of novel effective anti-cancer agents is imperative. Objective: The main objectives to synthesize new benzo[h]chromene derivatives and some reported derivatives then testing 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 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 Tubulin polymerization inhibitors using colchicines as standard drug; and molecular docking study for the most active derivative on these 2 enzymes was 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.