Synthesis and biological assay of erlotinib analogues and BSA-conjugated erlotinib analogue

Ramalingam Boobalan, Kuang Kai Liu, Jui-I Chao*, Chinpiao Chen

*Corresponding author for this work

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

A series of erlotinib analogues that have structural modification at 6,7-alkoxyl positions is efficiently synthesized. The in vitro anti-tumor activity of synthesized compounds is studied in two non-small cell lung cancer (NSCLC) cell lines (A549 and H1975). Among the synthesized compounds, the iodo compound 6 (ETN-6) exhibits higher anti-cancer activity compared to erlotinib. An efficient method is developed for the conjugation of erlotinib analogue-4, alcohol compound, with protein, bovine serum albumin (BSA), via succinic acid linker. The in vitro anti-tumor activity of the protein attached erlotinib analogue, 8 (ETN-4-Suc-BSA), showed stronger inhibitory activity in both A549 and H1975 NSCLC cell lines.

Original languageEnglish
Pages (from-to)1784-1788
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number8
DOIs
StatePublished - 1 Jan 2017

Keywords

  • Anti-cancer
  • BSA
  • EGFR
  • Erlotinib
  • NSCLC

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