The present study aims to evaluate phytochemical and pharmacological potentials of Dysphania ambrosioides (L.) Mosyakin & Clemants previously known as Chenopodium ambrosioides L. Extraction was carried out using 14 solvents with wide range of polarity to find out the best solvent system for each bioactivity. Total phenolic and flavonoids contents were measured colorimetrically and polyphenolics were quantified via HPLC-DAD analysis. The samples were screened for inhibitory potentials against free radicals, leishmania, cancer cell lines, protein kinase, α-Amylase enzymes and microbial strains. Among all solvents, maximum percentage of extract was recovered from methanol-water fraction of leaves. HPLC analysis exhibited the presence of rutin, myricetin and quercetin. In DPPH assay, methanolic leaf extract exhibited IC<sub>50</sub> value of 130.7 ± 0.57 μg/mL. Considerable α-amylase inhibitory, cytotoxic, leishmanicidal and antimicrobial potentials were exhibited by plant samples. D. ambrosioides revealed significant antioxidant, cytotoxic, antimicrobial and anti-diabetic potentials and thus warrant further detailed studies to find novel drugs.