Discovery of Antiglioma Activity of Biaryl 1,2,3,4-tetrahydroisoquinoline Derivatives and Conformationally Flexible Analogues.
From: Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, USA.
Journal of medicinal chemistry
- Publish Date: Sep 2006
- ISSN: 0022-2623
- Volume: 49
- Issue: 19
- Pages: 5845-8
- Medium: Print
- Language: English
- Citation (JAMA): Mohler Michael L, Kang Gyong-Suk, Hong Seoung-Soo, et al. Discovery of Antiglioma Activity of Biaryl 1,2,3,4-tetrahydroisoquinoline Derivatives and Conformationally Flexible Analogues.. J. Med. Chem. Sep 2006;49:5845-8
Abstract
Cultured rat astrocytes and C6 rat glioma were used as a differential screen for a variety of 1,2,3,4-tetrahydroisoquinoline (THI) derivatives. Compound 1 [1-(biphenyl-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol hydrochloride] selectively blocked the growth of C6 glioma leaving normal astrocytes relatively unaffected. The potential for clinical utility of 1 was further substantiated in human gliomas and other tumor cell lines. Preliminary SAR of this activity was characterized by synthesis and testing of several THI and conformationally flexible variants.
Mesh Headings (Keywords): Animals, Antineoplastic Agents, Astrocytes, Biphenyl Compounds, Cell Line, Tumor, Cells, Cultured, Drug Screening Assays, Antitumor, Glioma, Humans, Isoquinolines, Molecular Conformation, Rats, Structure-Activity Relationship, Tetrahydroisoquinolines
Check for Full Text / PubMed Unique Identifier (PMID): 16970409
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