叶酸、嘌呤、嘧啶拮抗剂在肿瘤治疗和核酸代谢的研究上占有重要地位。叶酸拮抗物(Folic acid antagonist)的研究至今不过十余年的历史,1936—1946年间Lewisohn 氏等曾用乳酸桿菌的发酵产物作用于小鼠自发性乳癌,可使1/3的癌肿消退。1944年 Hitchings 及其同事证实其作用成分为蝶氨苯甲酰三谷氨酸(Pteroyltriglutamicacid)。1946年 Angier 及 Subbarow 等合成此物质获得成功,叶酸及其衍生物的研究有了进一步的发展。1947年 Farber 及其同事试用蝶氨苯甲酰三谷氨酸(“teropterine”)及蝶氨 Folic acid, purine, pyrimidine antagonists play an important role in tumor therapy and nucleic acid metabolism research. Folic acid antagonist research to more than ten years until now, from 1936 to 1946 Lewisohn’s and other fermentation products of lactobacilli used in mouse spontaneous breast cancer, can make 1/3 of the cancer subsided. In 1944 Hitchings and colleagues confirmed that the active ingredient was Pteroyltriglutamic acid. The success of the synthesis of this material by Angier and Subbarow et al. In 1946 led to the further development of the study of folic acid and its derivatives. In 1947, Farber and colleagues tried “teropterine”