Renukadevi Patil, Shivaputra A Patil, Xiangdi Wang
2010
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Influential Citations
6
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Quality indicators
Journal
Medicinal Chemistry Research
Abstract
Novel tetrahydroisoquinoline (THI) analogs were designed, synthesized, and their antiglioma activity was evaluated. The results showed that 6,8-dimethoxy-1-(2′-methoxybiphenyl-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline hydrochloride (25) demonstrated improved potency, and selectivity on C6 rat glioma vs cultured rat astrocytes (EC50 0.63 μM vs. 10.85 μM) compared to our recent lead molecule EDL-155 (EC50 1.5 μM vs. 27.4 μM). The isomers of 25 were isolated using a semi-preparative high-performance liquid chromatography (HPLC) method, and their in vitro biological evaluation revealed that (+) 25 was the most active, and it was nearly 21 fold more potent than (−) 25, suggesting the antiglioma profile is influenced by stereochemical factors.