Discovery of a potent, metabolically stabilized resorcylic lactone as an anti-inflammatory lead

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6196-9. doi: 10.1016/j.bmcl.2009.08.096.

H Du ¹, T Matsushima, M Spyvee, M Goto, H Shirota, F Gusovsky, K Chiba, M Kotake, N Yoneda, Y Eguchi, L DiPietro, J-C Harmange, S Gilbert, X-Y Li, H Davis, Y Jiang, Z Zhang, R Pelletier, N Wong, H Sakurai, H Yang, H Ito-Igarashi, A Kimura, Y Kuboi, Y Mizui, I Tanaka, M Ikemori-Kawada, Y Kawakami, A Inoue, T Kawai, Y Kishi, Y Wang

Affiliations

Affiliation

1 Eisai Research Institute of Boston, 4 Corporate Drive, Andover, MA 01810, USA.

PMID: 19783437 DOI: 10.1016/j.bmcl.2009.08.096

Abstract

With bioactivity-guided phenotype screenings, a potent anti-inflammatory compound f152A1 has been isolated, characterized and identified as the known natural product LL-Z1640-2. Metabolic instability precluded its use for the study on animal disease models. Via total synthesis, a potent, metabolically stabilized analog ER-803064 has been created; addition of the (S)-Me group at C4 onto f152A1 has resulted in a dramatic improvement on its metabolic stability, while preserving the anti-inflammatory activities.

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