A review.Pyridine-based ring structures are widely employed in drug design due to their significant impact on pharmacol. activity, resulting in the development of various broad-spectrum therapeutics.The US FDA approves 95 pharmaceuticals derived from pyridine, including isoniazid and ethionamide for tuberculosis, delavirdine for HIV/AIDS, abiraterone acetate for prostate cancer, tacrine for Alzheimers, ciclopirox for ringworm and athletes foot, crizotinib for cancer, nifedipine for Raynauds syndrome and premature birth, piroxicam for arthritis, and nilvadipine for hypertension.Moreover, pyridine derivatives act as an excellent candidate for targeted anticancer agents.However, pyridine anti-cancer therapies continue to encounter hurdles, including poor response rates and drug resistance.Researchers are exploring pyridine derivatives as a potential treatment for targeted anticancer therapies.To further the development of targeted anti-cancer therapies, we analyzed pyridine-targeted drugs based on target categorization.We have covered all researchers of the last six years (2019-2024) investigating pyridine derivatives as targeted anticancer treatments.The highlights of pyridine-containing drugs and their targets are listed, as well as most promising drug candidates in clin. trials containing pyridine are also discussed.This review also included explanatory insights and viewpoints from several groups involved in the creation of targeted anticancer pyridine derivatives, with an emphasis on the structure-activity relationship (SAR).We hope that the current review provides insights and perspectives for the research and development of pyridine-containing anti-cancer drugs.