Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors
1
Mitsubishi Pharma Corporation, Pharmaceuticals Research Division, 1000, Kamoshida-cho, Aoba-ku, Yokohama 227-0033, Japan
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Publication type: Journal Article
Publication date: 2007-11-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
17869510
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
The present study identified several 4-alkynyl and 4-alkenylquinazolines that serve as novel and potent EGFR tyrosine kinase inhibitors. The IC(50) values of these compounds are in the nanomolar range. In addition, the 4-(4-phenylbut-1-yn/en-yl)quinazolines provided scaffolds for potent enzyme inhibition. Chiral discrimination was observed to occur in one of the 4-alkynylquinazoline derivatives with the (R)-isomer being more than 150 times as potent as the (S)-isomer.
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Kitano Y. et al. Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 21. pp. 5863-5867.
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Kitano Y., SUZUKI T., Kawahara E., Yamazaki T. Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors // Bioorganic and Medicinal Chemistry Letters. 2007. Vol. 17. No. 21. pp. 5863-5867.
Cite this
RIS
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TY - JOUR
DO - 10.1016/j.bmcl.2007.08.020
UR - https://doi.org/10.1016/j.bmcl.2007.08.020
TI - Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Kitano, Yasunori
AU - SUZUKI, TSUYOSHI
AU - Kawahara, Eiji
AU - Yamazaki, Takahisa
PY - 2007
DA - 2007/11/01
PB - Elsevier
SP - 5863-5867
IS - 21
VL - 17
PMID - 17869510
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
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@article{2007_Kitano,
author = {Yasunori Kitano and TSUYOSHI SUZUKI and Eiji Kawahara and Takahisa Yamazaki},
title = {Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2007},
volume = {17},
publisher = {Elsevier},
month = {nov},
url = {https://doi.org/10.1016/j.bmcl.2007.08.020},
number = {21},
pages = {5863--5867},
doi = {10.1016/j.bmcl.2007.08.020}
}
Cite this
MLA
Copy
Kitano, Yasunori, et al. “Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.” Bioorganic and Medicinal Chemistry Letters, vol. 17, no. 21, Nov. 2007, pp. 5863-5867. https://doi.org/10.1016/j.bmcl.2007.08.020.