Synthesis of thiophenecarboxamides, thieno [3, 4-c] pyridin-4 (5H)-ones and thieno [3, 4-d] pyrimidin-4 (3H)-ones and preliminary evaluation as inhibitors of poly (ADP …

AE Shinkwin, WJD Whish, MD Threadgill

文献索引：Shinkwin, Anne E.; Whish, William J. D.; Threadgill, Michael D. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 2 p. 297 - 308

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被引用次数: 40

摘要

Inhibitors of poly (ADP-ribose) polymerase (PARP) inhibit repair of damaged DNA and thus potentiate radiotherapy and chemotherapy of cancer. Treatment of 3-cyanothiophene with potassium nitrate and concentrated sulphuric acid gave 5-nitrothiophene-3-carboxamide. 4- Nitrothiophene-2-carboxamide and 5-nitrothiophene-2-carboxamide were formed similarly from 2-cyanothiophene. Reduction with tin (II) chloride gave the corresponding ...