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2005
Fused pyrimidine derivatives
R 0515
Novel 2-Amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as NonAntifolate Inhibitors of Thymidylate Synthase. — A variety of novel
36- 153 classical
5-arylthiopyrrolopyrimidines (V) (17 examples) are synthesized and evaluated as inhibitors of thymidylate synthase (TS) and as antitumor agents. Derivatives (Vd), (Ve)
and (Vf) are potent inhibitors of human TS and are more potent than clinically used
drugs ZD 1694 and LY231514 against human TS. — (GANGJEE*, A.; JAIN, H. D.;
KISLIUK, R. L.; Bioorg. Med. Chem. Lett. 15 (2005) 9, 2225-2230; Div. Med.
Chem., Grad. Sch. Pharm. Sci., Duquesne Univ., Pittsburgh, PA 15282, USA; Eng.)
— R. Langenstrassen
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