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Bioorg Med Chem Lett. 2005 Oct 1;15(19):4221-5.

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

Author information

1
Medicinal Chemistry Research Laboratories, 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. junya_ishida@po.fujisawa.co.jp

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.

PMID:
16098744
DOI:
10.1016/j.bmcl.2005.06.094
[Indexed for MEDLINE]

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