The effect of 1–4 on the expression of the pro-inflammatory inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) proteins in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells and the cytotoxicity of compounds 1–5 against a panel of cancer cell lines including human liver carcinoma (HepG2 and HepG3), human breast carcinoma (MCF-7 and MDA-MB-231), and human lung carcinoma (A-549) were evaluated in order to discover bioactive natural products. The gene discussed is PTGS2; the disease is cancer.