Abstract
A general protocol for the asymmetric synthesis of 3-N-arylmethylated right-half model compounds of renieramycins was developed, which enabled structure–activity relationship (SAR) study of several 3-N-arylmethyl derivatives. The most active compound (6a) showed significant cytotoxic activity against human prostate cancer DU145 and colorectal cancer HCT116 cell lines (IC50 = 11.9, and 12.5 nM, respectively).
Highlights
Natural products belonging to the bis-1,2,3,4-tetrahydroisoquinoline family, such as Natural products belonging to the bis-1,2,3,4-tetrahydroisoquinoline family, such as renieramycins, renieramycins, saframycins, and ecteinascidins, have attracted considerable attention due to their saframycins, and ecteinascidins, have attracted considerable attention due to their potent biological potent biological activities, structural diversity, and meager availability nature (Figure1) [1]
We have discovered a have discovered a number of renieramycin marine natural products having extraordinary structures number of renieramycin marine natural products having extraordinary structures from blue sponges from blue sponges collected inPhilippines
We have been developing a total synthesis of these fascinating marine
Summary
Received: 4 December 2018; Accepted: 17 December 2018; Published: 20 December 2018. Abstract:AAgeneral generalprotocol protocol for for the asymmetric compoundsofofrenieramycins renieramycinswas was developed, developed, which enabled compounds enabled structure–activity structure–activityrelationship relationship(SAR). (6a)showed showedsignificant significant cytotoxicactivity activityagainst against human prostate cancer
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