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Discovery, Total Synthesis, HRV 3C-protease Inhibitory Activity, and Structure-Activity Relationships of 2-methoxystypandrone and Its Analogues

S B Singh, P L Graham, R A Reamer, M G Cordingley

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3143-6.

PMID: 11720861

Abstract:

2-Methoxystypandrone, a naphthoquinone, was isolated from a Chinese herb Polygonum cuspidatum by bioassay guided fractionation using HRV 3C-protease assay. It showed an IC(50) value of 4.6 microM and is moderately selective. A new 10-step, total synthesis of 2-methoxystypandrone was accomplished in 45% overall yield using a Diels-Alder approach. Several analogues of this compound were prepared. Isolation, synthesis and HRV 3C-protease structure-activity relationships of these compounds have been described.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR42412301 HRV-3C Protease. HRV-3C Protease. Price
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