简洁且以多样性为导向的嵌入有优势苯并吡喃基序的新型支架的合成。

Concise and diversity-oriented synthesis of novel scaffolds embedded with privileged benzopyran motif.

作者信息

Ko Sung Kon, Jang Hwan Jong, Kim Eunha, Park Seung Bum

机构信息

School of Chemistry, Seoul National University, Seoul, 151-747, Korea.

出版信息

Chem Commun (Camb). 2006 Jul 28(28):2962-4. doi: 10.1039/b606341a. Epub 2006 Jun 13.

DOI:10.1039/b606341a

PMID:16832504

Abstract

A branching DOS strategy for an unbiased natural product-like library with embedded privileged benzopyran motif was established to provide complexity and diversity of resulting heterocycles with desired drug-likeness. The importance of skeletal diversity conducted on a privileged substructure was demonstrated through the biological evaluation of a small molecule library representing 22 unique core skeletons via in vitro cytotoxicity assay.

摘要

建立了一种用于具有嵌入式特权苯并吡喃基序的无偏类天然产物库的分支DOS策略，以提供具有所需药物相似性的所得杂环的复杂性和多样性。通过对代表22种独特核心骨架的小分子库进行体外细胞毒性试验的生物学评估，证明了在特权亚结构上进行骨架多样性的重要性。