Bioorganic & medicinal chemistry

Synthesis and in vitro antitumor activity of thiophene analogues of 5-chloro-5, 8-dideazafolic acid and 2-methyl-2-desamino-5-chloro-5, 8-dideazafolic acid

RA Forsch, JE Wright, A Rosowsky

Index: Forsch, Ronald A.; Wright, Joel E.; Rosowsky, Andre Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 6 p. 2067 - 2076

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Citation Number: 16

Abstract

N-[5-[N-(2-Amino-5-chloro-3, 4-dihydro-4-oxoquinazolin-6-yl) methylamino]-2-thenoyl]-l- glutamic acid (6) and N-[5-[N-(5-chloro-3, 4-dihydro-2-methyl-4-oxoquinazolin-6-yl) methylamino]-2-thenoyl]-l-glutamic acid (7), the first reported thiophene analogues of 5- chloro-5, 8-dideazafolic acid, were synthesized and tested as inhibitors of tumor cell growth in culture. 4-Chloro-5-methylisatin (10) was converted stepwise to methyl 2-amino-5- ...