Synthesis and biological evaluation of pyridooxazine-tetrahydroisoquinoline derivatives as MDR modulators

Chen Ma, Shao Jie Liu, Liang Xin, Qun Zhang, Kai Ding, J R Falck, Dong Soo Shin

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

Pyridooxazine-tetrahydroisoquinoline derivatives were designed and synthesized for MDR modulating activity. Pyridooxazin-2-one scaffolds were constructed in a one-pot annulation of N-substituted-2-chloroacetamides with 2-bromo-3-hydroxy pyridine via Smiles rearrangement. The Pictet-Spengler cyclization to form tetrahydroisoquinoline ring afforded target compounds in 17-37% overall yields. Some of these compounds exhibited multidrug resistance (MDR) reversing activity.

Original languageEnglish (US)
Pages (from-to)1010-1011
Number of pages2
JournalChemistry Letters
Volume35
Issue number9
DOIs
StatePublished - Sep 5 2006

ASJC Scopus subject areas

  • Chemistry(all)

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