Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products

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 agains...

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Autores principales: Matsubara, Takehiro, Yokoya, Masashi, Sirimangkalakitti, Natchanun, Saito, Naoki
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6356950/
https://www.ncbi.nlm.nih.gov/pubmed/30577460
http://dx.doi.org/10.3390/md17010003
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author Matsubara, Takehiro
Yokoya, Masashi
Sirimangkalakitti, Natchanun
Saito, Naoki
author_facet Matsubara, Takehiro
Yokoya, Masashi
Sirimangkalakitti, Natchanun
Saito, Naoki
author_sort Matsubara, Takehiro
collection PubMed
description 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 (IC(50) = 11.9, and 12.5 nM, respectively).
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spelling pubmed-63569502019-02-05 Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products Matsubara, Takehiro Yokoya, Masashi Sirimangkalakitti, Natchanun Saito, Naoki Mar Drugs Article 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 (IC(50) = 11.9, and 12.5 nM, respectively). MDPI 2018-12-20 /pmc/articles/PMC6356950/ /pubmed/30577460 http://dx.doi.org/10.3390/md17010003 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Matsubara, Takehiro
Yokoya, Masashi
Sirimangkalakitti, Natchanun
Saito, Naoki
Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
title Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
title_full Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
title_fullStr Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
title_full_unstemmed Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
title_short Asymmetric Synthesis and Cytotoxicity Evaluation of Right-Half Models of Antitumor Renieramycin Marine Natural Products
title_sort asymmetric synthesis and cytotoxicity evaluation of right-half models of antitumor renieramycin marine natural products
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6356950/
https://www.ncbi.nlm.nih.gov/pubmed/30577460
http://dx.doi.org/10.3390/md17010003
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