Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
oleh: Takehiro Matsubara, Masashi Yokoya, Natchanun Sirimangkalakitti, Naoki Saito
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2018-12-01 |
Deskripsi
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).