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2005
Fused pyrimidine derivatives
R 0515
Synthesis of 2-Amino-4-oxo-5-substitutedbenzylthiopyrrolo[2,3-d]pyrimidines as
Inhibitors of Thymidylate Synthase. — A series of thiopyrrolo[2,3-d]py27- 157 Potential
rimidine derivatives of type (V) is prepared as potential inhibitors of thymidylate synthase and as antitumor agents. Compound (Vc) is the most potent inhibitor. Contrary to
the analogues with an arylthio substituent in the 5-position, the substituents in the benzylthio group in (V) have little or no influence on the human thymidylate synthase inhibitory activity. — (GANGJEE*, A.; JAIN, H. D.; PHAN, J.; KISLIUK, R. L.;
J. Heterocycl. Chem. 42 (2005) 1, 165-168; Div. Med. Chem., Grad. Sch. Pharm. Sci.,
Duquesne Univ., Pittsburgh, PA 15282, USA; Eng.) — M. Bohle
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