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Design, Synthesis, and Evaluation of Ribose-Modified Anilinopyrimidine Derivatives as EGFR Tyrosine Kinase Inhibitors

Overview of attention for article published in Frontiers in Chemistry, November 2017
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Title
Design, Synthesis, and Evaluation of Ribose-Modified Anilinopyrimidine Derivatives as EGFR Tyrosine Kinase Inhibitors
Published in
Frontiers in Chemistry, November 2017
DOI 10.3389/fchem.2017.00101
Pubmed ID
Authors

Xiuqin Hu, Disha Wang, Yi Tong, Linjiang Tong, Xia Wang, Lili Zhu, Hua Xie, Shiliang Li, You Yang, Yufang Xu

Abstract

The synthesis of a series of ribose-modified anilinopyrimidine derivatives was efficiently achieved by utilizing DBU or tBuOLi-promoted coupling of ribosyl alcohols with 2,4,5-trichloropyrimidine as key step. Preliminary biological evaluation of this type of compounds as new EGFR tyrosine kinase inhibitors for combating EGFR L858R/T790M mutant associated with drug resistance in the treatment of non-small cell lung cancer revealed that 3-N-acryloyl-5-O-anilinopyrimidine ribose derivative 1a possessed potent and specific inhibitory activity against EGFR L858R/T790M over WT EGFR. Based upon molecular docking studies of the binding mode between compound 1a and EGFR, the distance between the Michael receptor and the pyrimidine scaffold is considered as an important factor for the inhibitory potency and future design of selective EGFR tyrosine kinase inhibitors against EGFR L858R/T790M mutants.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 9 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 9 100%

Demographic breakdown

Readers by professional status Count As %
Student > Bachelor 2 22%
Professor 1 11%
Student > Master 1 11%
Researcher 1 11%
Professor > Associate Professor 1 11%
Other 0 0%
Unknown 3 33%
Readers by discipline Count As %
Engineering 2 22%
Computer Science 1 11%
Biochemistry, Genetics and Molecular Biology 1 11%
Chemistry 1 11%
Medicine and Dentistry 1 11%
Other 0 0%
Unknown 3 33%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 2. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 31 October 2020.
All research outputs
#14,958,596
of 23,007,887 outputs
Outputs from Frontiers in Chemistry
#1,201
of 6,008 outputs
Outputs of similar age
#192,253
of 324,977 outputs
Outputs of similar age from Frontiers in Chemistry
#14
of 52 outputs
Altmetric has tracked 23,007,887 research outputs across all sources so far. This one is in the 32nd percentile – i.e., 32% of other outputs scored the same or lower than it.
So far Altmetric has tracked 6,008 research outputs from this source. They receive a mean Attention Score of 2.0. This one has gotten more attention than average, scoring higher than 74% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 324,977 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 37th percentile – i.e., 37% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 52 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 65% of its contemporaries.