Title of article :
The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-D]pyrimidine based antifolates as antineoplastic and antiarthritic agents
Author/Authors :
Lynn S. Gossett، نويسنده , , Lillian L. Habeck، نويسنده , , Katherine A. Shackelford، نويسنده , , Laurane G. Mendelsohn، نويسنده , , Susan B. Gates، نويسنده , , John F. Worzalla، نويسنده , , Tracy D. Self، نويسنده , , Karla S. Theobald، نويسنده , , Sherri L. Andis، نويسنده , , Richard M. Schultz، نويسنده , , Chuan Shih، نويسنده ,
Abstract :
A new series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates 1–3 were synthesized through an efficient conversion of 2-pivaloyl-4-oxo-6-ethynylpyrido[2,3-d]pyrimidine 5 to the corresponding 4-amino analog 7 via the activated 1,2,4-triazole intermediate 6. Compound 7 was used as the key intermediate for the preparation of the final products. The detailed biological evaluation of these compounds both as antineoplastic and antiarthritic agents will be discussed.
