Enantioselective synthesis and proteasome inhibition of A-ring analogs of (-)-epigallocatechin gallate (EGCG), the active ingredient of green tea extract.

[摘要]：The A-ring analog (2R,3R)-I (R3' = R5' = OH) of (-)-EGCG, the active ingredient of green tea, and analog (2R,3R)-I (R3' = R5' = H) of natural catechin from Cistus salviifolius, as well as their (2S,3S)-enantiomers were synthesized. They showed proteasomal inhibitory activities under cell free conditions, at a potency lower than that of (-)-EGCG. The results suggest that the hydroxyl groups in A-ring of (-)-EGCG play a role in enhancing the activity. The per-O-acetylated derivs. of these compds. showed cytotoxic activities and proteasomal inhibition after cellular intake, presumably acting as pro-drugs.

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