Structure–activity relationships and optimisation of the selective MDR modulator 2-(3, 4-dimethoxyphenyl)-5-(9-fluorenylamino)-2-(methylethyl) pentanenitrile and its N …

S Dei, E Teodori, A Garnier-Suillerot, F Gualtieri…

Index: Dei; Teodori; Garnier-Suillerot; Gualtieri; Scapecchi; Budriesi; Chiarini Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 10 p. 2673 - 2682

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Citation Number: 18

Abstract

Several ring-substituted derivatives of previously studied MDR inhibitors 2-(3, 4- dimethoxyphenyl)-5-(9-fluorenylamino)-2-(methylethyl) pentanenitrile and 2-(3, 4- dimethoxyphenyl)-5-[(9-fluorenyl)-N-methylamino]-2-(methylethyl) pentanenitrile have been synthesised and studied with the aim of optimising activity and selectivity. The results show that MDR inhibition is scarcely sensitive to modulation of the electronic properties of the ...

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