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A new diaryl urea compound, D181, induces cell cycle arrest in the G1 and M phases by targeting receptor tyrosine kinases and the microtubule skeleton

Overview of attention for article published in Investigational New Drugs, November 2010
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Title
A new diaryl urea compound, D181, induces cell cycle arrest in the G1 and M phases by targeting receptor tyrosine kinases and the microtubule skeleton
Published in
Investigational New Drugs, November 2010
DOI 10.1007/s10637-010-9577-1
Pubmed ID
Authors

Jin Zhang, Jing Zhou, Xiaomei Ren, Yanyan Diao, Honglin Li, Hualiang Jiang, Ke Ding, Duanqing Pei

Abstract

Receptor tyrosine kinases (RTKs) modulate a variety of cellular events, including cell proliferation, differentiation, mobility and apoptosis. In addition, RTKs have been validated as targets for cancer therapies. Microtubules are another class of proven targets for many clinical anticancer drugs. Here, we report that 1-(4-chloro-3-(trifluoromethyl) phenyl)-3-(2-cyano-4-hydroxyphenyl)urea (D181) functions as both a receptor tyrosine kinase inhibitor and a tubulin polymerization enhancer. D181 displayed potent inhibitory activities against a panel of RTKs, including Flt3, VEGFR, cKit, FGFR1 and PDGFRβ. D181 also enhanced tubulin polymerization and modified the secondary structure of tubulin proteins to disrupt their dynamic instability. Because of synergistic cooperation, D181 strongly inhibited the proliferation of various cancer cell lines, induced LoVo cell cycle arrest in the G1 and M phases and suppressed tumor growth in nude mice bearing human LoVo and HT29 xenografts. Our studies have provided a new, promising lead compound and novel clues for multi-target anticancer drug design and development.

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The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 14 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 14 100%

Demographic breakdown

Readers by professional status Count As %
Other 2 14%
Student > Bachelor 2 14%
Student > Ph. D. Student 2 14%
Professor > Associate Professor 2 14%
Researcher 1 7%
Other 1 7%
Unknown 4 29%
Readers by discipline Count As %
Agricultural and Biological Sciences 3 21%
Pharmacology, Toxicology and Pharmaceutical Science 2 14%
Chemistry 2 14%
Medicine and Dentistry 2 14%
Biochemistry, Genetics and Molecular Biology 1 7%
Other 0 0%
Unknown 4 29%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. 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 12 June 2012.
All research outputs
#20,159,700
of 22,668,244 outputs
Outputs from Investigational New Drugs
#975
of 1,164 outputs
Outputs of similar age
#82,870
of 87,669 outputs
Outputs of similar age from Investigational New Drugs
#25
of 26 outputs
Altmetric has tracked 22,668,244 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,164 research outputs from this source. They receive a mean Attention Score of 4.7. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 26 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.