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2008 Anticancer activity X 0070 Design and Synthesis of Tetrahydroisoquinoline Derivatives as Potential Multi- drug Resistance Reversal Agents in Cancer. — The representative tetrahydroisoqui- noline derivative (I) is synthesized and evaluated in several assays of MDR reversal and cardiovascular activities in vitro and in vivo. This compound exhibits a well-de- fined trend in MDR reversal activities and might be active by directly modulating the function of P-gp or indirectly inhibiting the P-gp transport function through decreasing membrane lipid fluidity. Compound (I) has no vascular contractile activity. — (LI, Y.; ZHANG*, H.-B.; HUANG, W.-L.; LI, Y.-M.; Bioorg. Med. Chem. Lett. 18 (2008) 12, 3652-3655; Cent. Drug Discovery, Coll. Pharm., China Pharm. Univ., Nanjing 210009, Peop. Rep. China; Eng.) — H. Hoennerscheid 45- 222

ChemInform Abstract: Design and Synthesis of Tetrahydroisoquinoline Derivatives as Potential Multidrug Resistance Reversal Agents in Cancer

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Page 1: ChemInform Abstract: Design and Synthesis of Tetrahydroisoquinoline Derivatives as Potential Multidrug Resistance Reversal Agents in Cancer

2008

Anticancer activityX 0070 Design and Synthesis of Tetrahydroisoquinoline Derivatives as Potential Multi-

drug Resistance Reversal Agents in Cancer. — The representative tetrahydroisoqui-noline derivative (I) is synthesized and evaluated in several assays of MDR reversal and cardiovascular activities in vitro and in vivo. This compound exhibits a well-de-fined trend in MDR reversal activities and might be active by directly modulating the function of P-gp or indirectly inhibiting the P-gp transport function through decreasing membrane lipid fluidity. Compound (I) has no vascular contractile activity. — (LI, Y.; ZHANG*, H.-B.; HUANG, W.-L.; LI, Y.-M.; Bioorg. Med. Chem. Lett. 18 (2008) 12, 3652-3655; Cent. Drug Discovery, Coll. Pharm., China Pharm. Univ., Nanjing 210009, Peop. Rep. China; Eng.) — H. Hoennerscheid

45- 222