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Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
ISSN: 1596-5996
EISSN: 1596-5996
Vol. 15, No. 11, 2016, pp. 2337-2343
Bioline Code: pr16308
Full paper language: English
Document type: Research Article
Document available free of charge

Tropical Journal of Pharmaceutical Research, Vol. 15, No. 11, 2016, pp. 2337-2343

 en Inhibitory activity of benzo[h]quinoline and benzo[h]chromene in human glioblastoma cells
Haiba, Mogedda E; Abdullah, Ebtehal S Al-; Ghabbour, Hazem A; Riyadh, Sayed M & Abdel-Kader, Reham M


Purpose: To carry out a neat synthesis of 2-amino-5,6-dihydro-8-methoxy-4-phenylbenzo[h]quinoline-3-carbonitrile (compound 2) and 2-amino-5,6-dihydro-8-methoxy-4-phenyl-4H-benzo[h]chromene-3-carbonitrile (compound 3) and evaluate their cytotoxic activity in human glioblastoma cells.
Methods: Benzo[h]quinoline and benzo[h]chromene were synthesized by treating 6-methoxy-1-tetralone with benzylidenemalononitrile under microwave irradiation. The structures of compounds 2 and 3 were confirmed by elemental, spectral, and x-ray crystallographic analyses. The cytotoxic activity of compounds 2 and 3 was evaluated using WST-1 assay in U373 human glioblastoma cell line.
Results: The molecular structures of compounds 2 and 3 were demonstrated unambiguously from single crystal x-ray measurements and they crystallized in triclinic form, P-1, for both compounds. In-vitro cytotoxic activity data for compound 2 in human glioblastoma cell line (U373) indicate that no significant cytotoxicity was observed. On the other hand, compound 3 showed highly significant cytotoxic effects on U373 cells at concentrations starting from 0.1 μg/ mL.
Conclusion: Compound 3 produces a decrease in cell viability with approximately 80 % cell death while compound 2 did not indicate significant cytotoxic activity. This suggests that the chromene moiety of compound 3 may be responsible for its high cytotoxicity.

Hydronaphthaline; Benzo[h]quinolone; Benzo[h]chromene; X-ray crystallography; U373 human glioblastoma; Cytotoxicity; Chromene moiety

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