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Design, Synthesis and Biological Activity Evaluation of S-Substituted 1H-5-Mercapto-1,2,4-Triazole Derivatives as Antiproliferative Agents in Colorectal Cancer

Overview of attention for article published in Frontiers in Chemistry, August 2018
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Title
Design, Synthesis and Biological Activity Evaluation of S-Substituted 1H-5-Mercapto-1,2,4-Triazole Derivatives as Antiproliferative Agents in Colorectal Cancer
Published in
Frontiers in Chemistry, August 2018
DOI 10.3389/fchem.2018.00373
Pubmed ID
Authors

Marius Mioc, Sorin Avram, Vasile Bercean, Ludovic Kurunczi, Roxana M. Ghiulai, Camelia Oprean, Dorina E. Coricovac, Cristina Dehelean, Alexandra Mioc, Mihaela Balan-Porcarasu, Calin Tatu, Codruta Soica

Abstract

Colon cancer is a widespread pathology with complex biochemical etiology based on a significant number of intracellular signaling pathways that play important roles in carcinogenesis, tumor proliferation and metastasis. These pathways function due to the action of key enzymes that can be used as targets for new anticancer drug development. Herein we report the synthesis and biological antiproliferative evaluation of a series of novel S-substituted 1H-3-R-5-mercapto-1,2,4-triazoles, on a colorectal cancer cell line, HT-29. Synthesized compounds were designed by docking based virtual screening (DBVS) of a previous constructed compound library against protein targets, known for their important role in colorectal cancer signaling: MEK1, ERK2, PDK1, VEGFR2. Among all synthesized structures, TZ55.7, which was retained as a possible PDK1 (phospholipid-dependent kinase 1) inhibitor, exhibited the most significant cytotoxic activity against HT-29 tumor cell line. The same compound alongside other two, TZ53.7 and TZ3a.7, led to a significant cell cycle arrest in both sub G0/G1 and G0/G1 phase. This study provides future perspectives for the development of new agents containing the 1,2,4-mercapto triazole scaffold with antiproliferative activities in colorectal cancer.

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Mendeley readers

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The data shown below were compiled from readership statistics for 35 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 35 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 7 20%
Student > Master 4 11%
Lecturer 3 9%
Student > Bachelor 3 9%
Other 2 6%
Other 6 17%
Unknown 10 29%
Readers by discipline Count As %
Chemistry 6 17%
Pharmacology, Toxicology and Pharmaceutical Science 4 11%
Veterinary Science and Veterinary Medicine 2 6%
Biochemistry, Genetics and Molecular Biology 2 6%
Agricultural and Biological Sciences 2 6%
Other 3 9%
Unknown 16 46%
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 23 August 2018.
All research outputs
#20,530,891
of 23,100,534 outputs
Outputs from Frontiers in Chemistry
#2,950
of 6,040 outputs
Outputs of similar age
#291,244
of 334,232 outputs
Outputs of similar age from Frontiers in Chemistry
#90
of 192 outputs
Altmetric has tracked 23,100,534 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 6,040 research outputs from this source. They receive a mean Attention Score of 2.0. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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 334,232 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 192 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.