Synthesis and in vitro evaluation of novel 1,2,3,4-tetrahydroisoquinoline derivatives as potent antiglioma agents

Renukadevi Patil, Amira Hosni-Ahmed, Terreia S. Jones, Shivaputra A. Patil, Likeselam B. Asres, Xiangdi Wang, Charles Yates, Eldon E. Geisert, Duane Miller

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Glioblastoma Multiforme (GBM) continues to demand improved chemotherapeutic solutions. In order to discover novel chemotherapeutic agents for GBM, we identified novel tetrahydroisoquinoline (THI) analogs as antiglioma agents. The present study reports the design, synthesis and in vitro evaluation of new THI derivatives in four established human glioma cell lines (T98, U87, LN18 and A172). Our structure activity relationship (SAR) studies revealed that the important modification of the carbon linker between the biphenyl and THI ring yielded EDL-360 (12) as a potent antiglioma agent (LN18; IC50: 5.42 ±0.06 uM) and is considered to be our new lead drug candidate for further preclinical studies.

Original languageEnglish (US)
Pages (from-to)473-482
Number of pages10
JournalAnti-Cancer Agents in Medicinal Chemistry
Volume14
Issue number3
DOIs
StatePublished - Feb 25 2014

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Tetrahydroisoquinolines
Glioblastoma
Structure-Activity Relationship
Glioma
Inhibitory Concentration 50
Carbon
Cell Line
Pharmaceutical Preparations
1,2,3,4-tetrahydroisoquinoline
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Pharmacology
  • Cancer Research

Cite this

Synthesis and in vitro evaluation of novel 1,2,3,4-tetrahydroisoquinoline derivatives as potent antiglioma agents. / Patil, Renukadevi; Hosni-Ahmed, Amira; Jones, Terreia S.; Patil, Shivaputra A.; Asres, Likeselam B.; Wang, Xiangdi; Yates, Charles; Geisert, Eldon E.; Miller, Duane.

In: Anti-Cancer Agents in Medicinal Chemistry, Vol. 14, No. 3, 25.02.2014, p. 473-482.

Research output: Contribution to journalArticle

Patil, Renukadevi ; Hosni-Ahmed, Amira ; Jones, Terreia S. ; Patil, Shivaputra A. ; Asres, Likeselam B. ; Wang, Xiangdi ; Yates, Charles ; Geisert, Eldon E. ; Miller, Duane. / Synthesis and in vitro evaluation of novel 1,2,3,4-tetrahydroisoquinoline derivatives as potent antiglioma agents. In: Anti-Cancer Agents in Medicinal Chemistry. 2014 ; Vol. 14, No. 3. pp. 473-482.
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