Discovery, total synthesis, HRV 3C-protease inhibitory activity, and structure–activity relationships of 2-methoxystypandrone and its analogues

SB Singh, PL Graham, RA Reamer… - Bioorganic & medicinal …, 2001 - Elsevier
2-Methoxystypandrone, a naphthoquinone, was isolated from a Chinese herb Polygonum
cuspidatum by bioassay guided fractionation using HRV 3C-protease assay. It showed an
IC50 value of 4.6 μM 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.

[引用][C] Discovery, total synthesis, HRV 3C-protease inhibitory activity, and structure-activity relationships of 2-methoxystypandrone and its analogues

S SB - Bioorg Med Chem Lett, 2001 - cir.nii.ac.jp
Discovery, total synthesis, HRV 3C-protease inhibitory activity, and structure-activity
relationships of 2-methoxystypandrone and its analogues | CiNii Research … Discovery,
total synthesis, HRV 3C-protease inhibitory activity, and structure-activity relationships of 2-methoxystypandrone
and its analogues
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