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M. Paul Gleeson. Design, synthesis and biological evaluation of covalent inhibitor of epidermal growth factor receptor (EGFR) kinase. (). King Mongkut's University of Technology North Bangkok. Central Library. : , 2019.
Design, synthesis and biological evaluation of covalent inhibitor of epidermal growth factor receptor (EGFR) kinase
Name: Nicharee Jiracheep
Organization :
King Mongkut's Institute of Technology Ladkrabang. Faculty of Engineering
Name: Borvornwat Toviwek
Organization :
Kasetsart University. Faculty of Science
Name: Nattanan Jiwacharoenchai
Organization :
Kasetsart University. Faculty of Science
Name: Supa Hannongbua
Organization :
Kasetsart University. Faculty of Science
Name: Kiattawee Choowongkomon
Organization :
Kasetsart University. Faculty of Science
Name: M. Paul Gleeson
Organization :
King Mongkut's Institute of Technology Ladkrabang. Faculty of Engineering
Email :
paul.gl@kmitl.ac.th
keyword:
Covalent inhibitors
LCSH:
HER-2 gene
Abstract:
Epidermal growth factor receptors (EGFRs) are a large family of tyrosine kinases implicated in the uncontrolled growth of non-small cell lung cancer (NSCLC). In this work, we report the initial results related to the preparation and testing of novel covalent pyrimidine-based EGFR inhibitors. Compounds have been prepared using Pd-catalysed Suzuki coupling reactions of aryl boronic acids at the 2-position of 2,4-dichloropyrimidine followed by the acid-catalysed substitution of anilino reagents at the 2-position. A Michael acceptor group was included at the 4-position of compound 8 as part of our initial development efforts. We have evaluated compounds in an EGFR kinase biochemical assays and in-vitro cell lines (A431) to determine their potential as therapeutic agents. The compound was then compared to known EGFR drugs Erlotinib and Afatinib. Molecular modelling has been used to predict the most probable binding mode within the ATP binding site. Our chemotype is predicted to form a covalent adduct between Cysteine 797 and the inhibitor Michael acceptor moiety. The goal of this work is to better understand how these suicidal inhibitors function, and therefore further improved and how selectivity can be obtained over other kinases. With this preliminary information, the design of cheaper and potentially more selective and more effective inhibitors will be possible
King Mongkut's University of Technology North Bangkok. Central Library
Address:
BANGKOK
Email:
library@kmutnb.ac.th
Created:
2019
Modified:
2019-10-10
Issued:
2019-10-10
บทความ/Article
application/pdf
BibliograpyCitation :
In Chemical Society of Thailand under the Patronage of Professor Dr. HRH Princess Chulabhorn. Pure and Applied Chemistry International Conference 2019 (PACCON 2019) (OR21-26). Bangkok : Mahidol University
eng
©copyrights King Mongkut's University of Technology North Bangkok
RightsAccess:
ใช้เวลา
0.050556 วินาที
Nicharee Jiracheep
| Title | Contributor | Type |
|---|---|---|
| Design, synthesis and biological evaluation of covalent inhibitor of epidermal growth factor receptor (EGFR) kinase
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Nicharee Jiracheep;Borvornwat Toviwek;Nattanan Jiwacharoenchai;Supa Hannongbua;Kiattawee Choowongkomon;M. Paul Gleeson | บทความ/Article |
Borvornwat Toviwek
| Title | Contributor | Type |
|---|---|---|
| Design, synthesis and biological evaluation of covalent inhibitor of epidermal growth factor receptor (EGFR) kinase
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Nicharee Jiracheep;Borvornwat Toviwek;Nattanan Jiwacharoenchai;Supa Hannongbua;Kiattawee Choowongkomon;M. Paul Gleeson | บทความ/Article | |
| Design, synthesis, biological and computational evaluation of novel 4-aryl-N-phenylpyrimidin-2-amines and N2, N4 - diarylpyrimidine-2,4- diamine inhibitors of protein kinases
มหาวิทยาลัยเกษตรศาสตร์ Borvornwat Toviwek | Matthew Paul Gleeson | วิทยานิพนธ์/Thesis |
Nattanan Jiwacharoenchai
| Title | Contributor | Type |
|---|---|---|
| Design, synthesis and biological evaluation of covalent inhibitor of epidermal growth factor receptor (EGFR) kinase
มหาวิทยาลัยเทคโนโลยีพระจอมเกล้าพระนครเหนือ Nicharee Jiracheep;Borvornwat Toviwek;Nattanan Jiwacharoenchai;Supa Hannongbua;Kiattawee Choowongkomon;M. Paul Gleeson | บทความ/Article |
Supa Hannongbua
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| Title | Contributor | Type |
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