4-Phenyl-1, 2, 3, 6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors

…, K Hattori, H Yamamoto, A Iwashita, K Mihara…

Index: Ishida, Junya; Hattori, Kouji; Yamamoto, Hirofumi; Iwashita, Akinori; Mihara, Kayoko; Matsuoka, Nobuya Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 19 p. 4221 - 4225

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Citation Number: 35

Abstract

We have shown that a 4-phenyl-1, 2, 3, 6-tetrahydropyridine fragment plays an important role in improving inhibitory potency against poly (ADP-ribose) polymerase-1 (PARP-1). Various benzamide analogues linked with this fragment via alkyl spacers have been prepared and evaluated. As a result, some of them have been found to be highly potent PARP-1 inhibitors.