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

Abstract

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.

Pyrimidines as Anticancer and Antiviral: Synthesis & Reactions (A Review)

“…One year later, we prepared 50 fused pyrimidine analogues 47 and 48 and assigned their anticancer activity against nine types of cancer on approximate sixty cell lines via the reaction of 2-amino-3-cyanochromenes with either formic acid or formamide (Scheme 17).…”