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

Ramalingam Boobalan; Kuang Kai Liu; Jui-I Chao; Chinpiao Chen

doi:10.1016/j.bmcl.2017.02.059

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

Institute of Molecular Medicine and Bioengineering

Research output: Contribution to journal › Article › peer-review

10 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 language	English
Pages (from-to)	1784-1788
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	27
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2017.02.059
State	Published - 2017

Keywords

Anti-cancer
BSA
EGFR
Erlotinib
NSCLC

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2017.02.059

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title = "Synthesis and biological assay of erlotinib analogues and BSA-conjugated erlotinib analogue",

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.",

keywords = "Anti-cancer, BSA, EGFR, Erlotinib, NSCLC",

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TY - JOUR

T1 - Synthesis and biological assay of erlotinib analogues and BSA-conjugated erlotinib analogue

AU - Boobalan, Ramalingam

AU - Liu, Kuang Kai

AU - Chao, Jui-I

AU - Chen, Chinpiao

PY - 2017

Y1 - 2017

N2 - 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.

AB - 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.

KW - Anti-cancer

KW - BSA

KW - EGFR

KW - Erlotinib

KW - NSCLC

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U2 - 10.1016/j.bmcl.2017.02.059

DO - 10.1016/j.bmcl.2017.02.059

M3 - Article

C2 - 28268137

AN - SCOPUS:85014241262

SN - 0960-894X

VL - 27

SP - 1784

EP - 1788

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 8

ER -

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

Abstract

Keywords

UN SDGs

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