Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines
Liu He
1
,
Bin Wu
1
,
YANG GE
1
,
Jiaxin Huang
1
,
Shijie Song
1
,
Changyuan Wang
1
,
Ji-hong Yao
1
,
Kexin Liu
1
,
Yanxia Li
2
,
Yongming Li
1
,
Xiaodong Ma
1
Publication type: Journal Article
Publication date: 2017-12-01
scimago Q2
wos Q1
SJR: 0.608
CiteScore: 6.7
Impact factor: 3.0
ISSN: 09680896, 14643391
PubMed ID:
29102081
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
A family of phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) were synthesized as potent focal adhesion kinase (FAK) inhibitors. The PA-DPPY derivatives could significantly inhibit the FAK enzymatic activity at concentrations lower than 10.69 nM. Among them, compounds 7a and 7e were two of the most active FAK inhibitors, possessing IC50 values of 4.25 nM and 4.65 nM, respectively. In particular, compound 7e also displayed strong activity against AsPC cell line, with an IC50 of 1.66 μM, but show low activity against the normal HPDE6-C7 cells (IC50 > 20 μM), indicating its low cell cytotoxicity. Additionally, flow cytometry analysis showed that after treatment with 7e (8 μM, 72 h), both AsPC and Panc cells growth were almost totally inhibited, with a cell viability rate of 16.8% and 18.1%, respectively. Overall, compound 7e may be served as a valuable FAK inhibitor for the treatment of pancreatic cancer.
Found
Nothing found, try to update filter.
Found
Nothing found, try to update filter.
Top-30
Journals
|
1
2
3
4
5
|
|
|
European Journal of Medicinal Chemistry
5 publications, 23.81%
|
|
|
Future Medicinal Chemistry
2 publications, 9.52%
|
|
|
Chemical Biology and Drug Design
2 publications, 9.52%
|
|
|
Current Medicinal Chemistry
1 publication, 4.76%
|
|
|
Molecules
1 publication, 4.76%
|
|
|
International Journal of Molecular Sciences
1 publication, 4.76%
|
|
|
Mendeleev Communications
1 publication, 4.76%
|
|
|
Bioorganic and Medicinal Chemistry
1 publication, 4.76%
|
|
|
Journal of Labelled Compounds and Radiopharmaceuticals
1 publication, 4.76%
|
|
|
Journal of Medicinal Chemistry
1 publication, 4.76%
|
|
|
Bioengineered
1 publication, 4.76%
|
|
|
Russian Journal of General Chemistry
1 publication, 4.76%
|
|
|
Expert Opinion on Therapeutic Patents
1 publication, 4.76%
|
|
|
RSC Advances
1 publication, 4.76%
|
|
|
Coordination Chemistry Reviews
1 publication, 4.76%
|
|
|
1
2
3
4
5
|
Publishers
|
1
2
3
4
5
6
7
|
|
|
Elsevier
7 publications, 33.33%
|
|
|
Taylor & Francis
4 publications, 19.05%
|
|
|
Wiley
3 publications, 14.29%
|
|
|
MDPI
2 publications, 9.52%
|
|
|
Bentham Science Publishers Ltd.
1 publication, 4.76%
|
|
|
OOO Zhurnal "Mendeleevskie Soobshcheniya"
1 publication, 4.76%
|
|
|
American Chemical Society (ACS)
1 publication, 4.76%
|
|
|
Pleiades Publishing
1 publication, 4.76%
|
|
|
Royal Society of Chemistry (RSC)
1 publication, 4.76%
|
|
|
1
2
3
4
5
6
7
|
- We do not take into account publications without a DOI.
- Statistics recalculated weekly.
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.
Metrics
21
Total citations:
21
Citations from 2025:
3
(14.28%)
Cite this
GOST |
RIS |
BibTex |
MLA
Cite this
GOST
Copy
He L. et al. Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines // Bioorganic and Medicinal Chemistry. 2017. Vol. 25. No. 24. pp. 6313-6321.
GOST all authors (up to 50)
Copy
He L., Wu B., GE Y., Huang J., Song S., Wang C., Yao J., Liu K., Li Y., Li Y., Ma X. Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines // Bioorganic and Medicinal Chemistry. 2017. Vol. 25. No. 24. pp. 6313-6321.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmc.2017.09.041
UR - https://doi.org/10.1016/j.bmc.2017.09.041
TI - Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines
T2 - Bioorganic and Medicinal Chemistry
AU - He, Liu
AU - Wu, Bin
AU - GE, YANG
AU - Huang, Jiaxin
AU - Song, Shijie
AU - Wang, Changyuan
AU - Yao, Ji-hong
AU - Liu, Kexin
AU - Li, Yanxia
AU - Li, Yongming
AU - Ma, Xiaodong
PY - 2017
DA - 2017/12/01
PB - Elsevier
SP - 6313-6321
IS - 24
VL - 25
PMID - 29102081
SN - 0968-0896
SN - 1464-3391
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2017_He,
author = {Liu He and Bin Wu and YANG GE and Jiaxin Huang and Shijie Song and Changyuan Wang and Ji-hong Yao and Kexin Liu and Yanxia Li and Yongming Li and Xiaodong Ma},
title = {Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines},
journal = {Bioorganic and Medicinal Chemistry},
year = {2017},
volume = {25},
publisher = {Elsevier},
month = {dec},
url = {https://doi.org/10.1016/j.bmc.2017.09.041},
number = {24},
pages = {6313--6321},
doi = {10.1016/j.bmc.2017.09.041}
}
Cite this
MLA
Copy
He, Liu, et al. “Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines.” Bioorganic and Medicinal Chemistry, vol. 25, no. 24, Dec. 2017, pp. 6313-6321. https://doi.org/10.1016/j.bmc.2017.09.041.