- 4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.
Bioorganic & medicinal chemistry letters (2005-08-16)
Junya Ishida, Kouji Hattori, Hirofumi Yamamoto, Akinori Iwashita, Kayoko Mihara, Nobuya Matsuoka
PMID16098744
要旨
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.
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