Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
A general protocol for the asymmetric synthesis of 3-<i>N</i>-arylmethylated right-half model compounds of renieramycins was developed, which enabled structure⁻activity relationship (SAR) study of several 3-<i>N</i>-arylmethyl derivatives. The most active compound (...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2018-12-01
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| Series: | Marine Drugs |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1660-3397/17/1/3 |
| Summary: | A general protocol for the asymmetric synthesis of 3-<i>N</i>-arylmethylated right-half model compounds of renieramycins was developed, which enabled structure⁻activity relationship (SAR) study of several 3-<i>N</i>-arylmethyl derivatives. The most active compound (<b>6a</b>) showed significant cytotoxic activity against human prostate cancer DU145 and colorectal cancer HCT116 cell lines (IC<sub>50</sub> = 11.9, and 12.5 nM, respectively). |
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| ISSN: | 1660-3397 |