<p>Background: The coumarin nuclei, which exist in many heterocyclic compounds, has gained a lot of
attention over the past decade due to their wide range of biological activities such as antibacterial, anticoagulant,
antiviral, antifungal, anticancer, and anti-inflammatory properties.
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<p>
Objective: The multi-component reactions of 5,5-dimethylcyclohexane-1,3-dione with acetophenone derivatives
and triethoxymethane produced biologically active target chromene molecules and their fused derivatives.
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<p>
Methods: The reaction of 5,5-dimethylcyclohexane-1,3-dione and each of triethoxymethane and acetophenone
derivatives 3a-g in absolute ethanol containing triethylamine gave the 4,6,7,8-tetrahydro-5H-chromen-5-one
derivatives 4a-g. Compounds 4a-d were used for further heterocyclization reactions to produce biologically active fused pyrazole, thiophene, and thiazole derivative corporate with the chromenes caffold.
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<p>
Results: The cytotoxicity of the synthesized compounds were evaluated using six cancer cell lines together with
c-Met kinase and PC-3 cell line inhibitions. In addition, cytotoxicity toward hepatocellular carcinoma HepG2 and
cervical carcinoma HeLa was carried out as well as the in-vitro cytotoxic potential for all compounds against
peripheral blood lymphocytes (PBL) extracted from healthy donors. Morphological changes of the A549 cell line
by the two most active compounds were also studied.
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<p>
Conclusion: The synthesized heterocyclic compounds were originally obtained from 5,5-dimethylcyclohexane1,3-dione. Several of the produced compounds exhibited high inhibitions toward several cancer cell lines proving
high inhibitions, therefore, encouraging further studies to synthesize heterocyclic compounds based on chromene
scaffold.</p>