Bioorganic & Medicinal Chemistry Letters 2005-10-01

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

Junya Ishida, Kouji Hattori, Hirofumi Yamamoto, Akinori Iwashita, Kayoko Mihara, Nobuya Matsuoka

Index: Bioorg. Med. Chem. Lett. 15(19) , 4221-5, (2005)

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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.