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

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分子醫學與生物工程研究所

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10 引文斯高帕斯（Scopus）

摘要

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.

原文	English
頁（從 - 到）	1784-1788
頁數	5
期刊	Bioorganic and Medicinal Chemistry Letters
卷	27
發行號	8
DOIs	https://doi.org/10.1016/j.bmcl.2017.02.059
出版狀態	Published - 2017

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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",

author = "Ramalingam Boobalan and Liu, {Kuang Kai} and Jui-I Chao and Chinpiao Chen",

note = "Publisher Copyright: {\textcopyright} 2017 Elsevier Ltd",

year = "2017",

doi = "10.1016/j.bmcl.2017.02.059",

language = "English",

volume = "27",

pages = "1784--1788",

journal = "Bioorganic and Medicinal Chemistry Letters",

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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

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