Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues

Michael L. Mohler, Gyong Suk Kang, Seoung Soo Hong, Renukadevi Patil, Oleg V. Kirichenko, Wei Li, Igor M. Rakov, Eldon E. Geisert, Duane Miller

Research output: Contribution to journalArticle

18 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)5845-5848
Number of pages4
JournalJournal of Medicinal Chemistry
Volume49
Issue number19
DOIs
StatePublished - Sep 21 2006

Fingerprint

Glioma
Astrocytes
Tetrahydroisoquinolines
Tumor Cell Line
Growth
1,2,3,4-tetrahydroisoquinoline
1-(biphenyl-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Cite this

Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues. / Mohler, Michael L.; Kang, Gyong Suk; Hong, Seoung Soo; Patil, Renukadevi; Kirichenko, Oleg V.; Li, Wei; Rakov, Igor M.; Geisert, Eldon E.; Miller, Duane.

In: Journal of Medicinal Chemistry, Vol. 49, No. 19, 21.09.2006, p. 5845-5848.

Research output: Contribution to journalArticle

Mohler, Michael L. ; Kang, Gyong Suk ; Hong, Seoung Soo ; Patil, Renukadevi ; Kirichenko, Oleg V. ; Li, Wei ; Rakov, Igor M. ; Geisert, Eldon E. ; Miller, Duane. / Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues. In: Journal of Medicinal Chemistry. 2006 ; Vol. 49, No. 19. pp. 5845-5848.
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