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The objective of the present study was the bioprospection of bioactive compounds from endophytic Thielaviopsis basicola with therapeutic applications, isolated from Ximenia americana, Western Ghats of Karnataka, India. The fresh and healthy leaves and roots of Ximenia americana were collected from the forests of Western Ghats of Karnataka, India. The collected explants were submerged for the enumeration and purification of fungal endophytes by using selective, and different media. Isolated fungal endophytes were processed for the production, extraction, phytochemical analysis, purification and evaluation of bioactive compounds by referring standard protocols. At a glance, endophyte derived bioactive compounds were used in in-vitro antagonistic, antioxidant antiurolithisis, and anticancer activity. A total of 32 pure isolates were obtained, 8 morphologically distinct fungal endophytes were identified from 200 explants of X. americana. Endophytic Thielaviopsis basicola was a core candidate identified and cultivated in solid-state fermentation on corn bran under the dark condition at 25° ± 2° for 15 days. Obtained 5.30g of aqueous crude extract per 100g of cornmeal were processed for qualitative phytochemical analysis, in alkaloids, terpenoids, flavonoids, phenols, tannins, and glycosides were found. The aqueous crude extract showed 0.761g of phenol and 0.276g of flavonoids content. From these crude extract TbCC1 and TbCC2, two fractions were purified by column chromatography and spotted potent bioactive compounds on thin layer chromatography. The FTIR data of TbCC1 and TbCC2 showed different functional groups such as alcohol, phenols, alkanes, alkenes, aromatic, alkyl halides, amines, ether, and nitrile. The TbCC1 exhibited prominent antagonistic activity and MIC against Staphylococcus aureus (24mm with 100µg/mL) and Candida albicans (22mm with 75µg/mL) while TbCC2 exhibited against Salmonella typhi (22mm with 75µg/mL) and Aspergillus fumigatus (18mm with 75µg/mL). The TbCC1 showed potent antioxidant activity (86.24±0.35) with 5.26µg/mL of IC50 value as compared with TbCC2. The maximum antiurolithiasis activity showed with 100% concentration at the rate of 67.5±1.49 of aqueous crude extract. The Sulphorodamine B assay showed MCF7 human breast cancer cell line viability 98.39±0.0250 at 100µg concentration and 40.81±0.0470 at 500µg with an IC50 value of 459.60µg. This is the first innovative report of endophytic Thielaviopsis basicola for their phytochemicals detection and prominent in-vitro activities from the selected plants. [ABSTRACT FROM AUTHOR]