Substituted 3- benzoyl flavone 4 was synthesized via modified Baker-Venkatraman reaction. The chemical structure of the newly synthesized compound was confirmed by ¹H NMR, MS, IR spectral data. LD₅₀valueof synthesized compound was determined on Acute Oral toxicity studies carried out as per OECD guidelines-423 and were found to be 200 mg/ kg body weight. The compound was screened for Anti-inflammatory (Carrageenen-induced rat paw edema model) and Anti-oxidant activity (DPPH-radical scavenging model) and Brine Shrimp cyto-toxicity assay. On screening, it was found that 3-benzoyl flavone with electron donating substitutions (4) has significant Anti-oxidant potential (IC₅₀ 19.75µg/ml) and Anti-inflammatory activity (% reduction in edema 83.75± 5.30 %). Compound 4 also has highest cyto-toxicity on Brine Shrimp Nauplii (IC₅₀ 0.45 mg/ml). Also, screening of anti-cancer activity on 60 cell lines of 9 different types of cancers by NCI – NIH showed that compound 4 is active against renal cancer (cell line UO-31).