Synthetic studies on isoquinoline derivatives with multidrug resistance (MDR) modulating activity

Chen Ma; Su Dong Cho; J R Falck; Dong Soo Shin

doi:10.3987/COM-03-9918

Synthetic studies on isoquinoline derivatives with multidrug resistance (MDR) modulating activity

Chen Ma, Su Dong Cho, J R Falck, Dong Soo Shin

Biochemistry

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

Abstract

Tetrahydropyridazino-1,4-oxazinoisoquinoline derivatives with multidrug Resist. (MDR) modulating activity were designed and synthesized. A key step for cyclization of 1,4-oxazine ring was developed using K₂CO₃ and CH₃CN in one-pot. Among prepared compounds, 2-(4-fluorobenzyl)-9,10-dimethoxy-12-methyl-6,7,11b,12-tetrahydropyridazino[4', 5',5,6] [1,4]oxazine-[3,4,-a]isoquinolin-1(2H)-one (1f) exhibited significant MDR reversing activity and low toxicity, which might be as potential MDR agent.

Original language	English (US)
Pages (from-to)	75-85
Number of pages	11
Journal	Heterocycles
Volume	63
Issue number	1
DOIs	https://doi.org/10.3987/COM-03-9918
State	Published - Jan 1 2004

ASJC Scopus subject areas

Analytical Chemistry
Pharmacology
Organic Chemistry

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abstract = "Tetrahydropyridazino-1,4-oxazinoisoquinoline derivatives with multidrug Resist. (MDR) modulating activity were designed and synthesized. A key step for cyclization of 1,4-oxazine ring was developed using K2CO3 and CH3CN in one-pot. Among prepared compounds, 2-(4-fluorobenzyl)-9,10-dimethoxy-12-methyl-6,7,11b,12-tetrahydropyridazino[4', 5',5,6] [1,4]oxazine-[3,4,-a]isoquinolin-1(2H)-one (1f) exhibited significant MDR reversing activity and low toxicity, which might be as potential MDR agent.",

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AB - Tetrahydropyridazino-1,4-oxazinoisoquinoline derivatives with multidrug Resist. (MDR) modulating activity were designed and synthesized. A key step for cyclization of 1,4-oxazine ring was developed using K2CO3 and CH3CN in one-pot. Among prepared compounds, 2-(4-fluorobenzyl)-9,10-dimethoxy-12-methyl-6,7,11b,12-tetrahydropyridazino[4', 5',5,6] [1,4]oxazine-[3,4,-a]isoquinolin-1(2H)-one (1f) exhibited significant MDR reversing activity and low toxicity, which might be as potential MDR agent.

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Synthetic studies on isoquinoline derivatives with multidrug resistance (MDR) modulating activity

Abstract

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