A new series of N-(3-(5-phenyl-1,3,4-oxadiazol-2-yl)phenyl)-2,4-dihydroxypyrimidine-5-sulfonamide derivatives was developed as dual TS and antiangiogenic agents.107 Among these, compound 1 emerged as the most potent TS inhibitor (IC50 = 0.11 μM), exhibiting pronounced selectivity toward non-small cell lung cancer (NSCLC) cell lines. Here, TYMS is linked to non-small cell lung carcinoma.