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The synthesis and biological activity of a series of 2,4-diaminopyrido[2,3-d]pyrimidine based antifolates as antineoplastic and antiarthritic agents.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gossett LS,Habeck LL,Shackelford KA,Mendelsohn LG,Gates SB,Worzalla JF,Self TD,Theobald KS,Andis SL,Schultz RM,Shih C

doi

10.1016/s0960-894x(98)00683-0

subject

Has Abstract

pub_date

1999-01-04 00:00:00

pages

75-8

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960894X98006830

journal_volume

9

pub_type

杂志文章

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