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Synthesis and anticancer activity of novel quinazolinone-based rhodanines

Overview of attention for article published in Chemistry Central Journal, October 2017
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Title
Synthesis and anticancer activity of novel quinazolinone-based rhodanines
Published in
Chemistry Central Journal, October 2017
DOI 10.1186/s13065-017-0333-x
Pubmed ID
Authors

Sherihan El-Sayed, Kamel Metwally, Abdalla A. El-Shanawani, Lobna M. Abdel-Aziz, Harris Pratsinis, Dimitris Kletsas

Abstract

Rhodanines and quinazolinones have been reported to possess various pharmacological activities. A novel series of twenty quinazolinone-based rhodanines were synthesized via Knoevenagel condensation between 4-[3-(substitutedphenyl)-3,4-dihydro-4-oxoquinazolin-2-yl)methoxy]substituted-benzaldehydes and rhodanine. Elemental and spectral analysis were used to confirm structures of the newly synthesized compounds. The newly synthesized compounds were biologically evaluated for in vitro cytotoxic activity against the human fibrosarcoma cell line HT-1080 as a preliminary screen using the MTT assay. All the target compounds were active, displaying IC50 values roughly in the range of 10-60 µM. Structure-activity relationship study revealed that bulky, hydrophobic, and electron withdrawing substituents at the para-position of the quinazolinone 3-phenyl ring as well as methoxy substitution on the central benzene ring, enhance cytotoxic activity. The four most cytotoxic compounds namely, 45, 43, 47, and 37 were further tested against two human leukemia cell lines namely, HL-60 and K-562 and showed cytotoxic activity in the low micromolar range with compound 45 being the most active, having IC50 values of 1.2 and 1.5 μM, respectively. Interestingly, all four compounds were devoid of cytotoxicity against normal human fibroblasts strain AG01523, indicating that the synthesized rhodanines may be selectively toxic against cancer cells. Mechanistic studies revealed that the most cytotoxic target compounds exhibit pro-apoptotic activity and trigger oxidative stress in cancer cells.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 31 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 31 100%

Demographic breakdown

Readers by professional status Count As %
Lecturer 5 16%
Researcher 3 10%
Student > Master 3 10%
Student > Doctoral Student 2 6%
Student > Bachelor 2 6%
Other 6 19%
Unknown 10 32%
Readers by discipline Count As %
Chemistry 9 29%
Pharmacology, Toxicology and Pharmaceutical Science 5 16%
Biochemistry, Genetics and Molecular Biology 4 13%
Agricultural and Biological Sciences 2 6%
Social Sciences 1 3%
Other 1 3%
Unknown 9 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 31 July 2021.
All research outputs
#21,158,537
of 25,988,468 outputs
Outputs from Chemistry Central Journal
#255
of 410 outputs
Outputs of similar age
#263,829
of 339,111 outputs
Outputs of similar age from Chemistry Central Journal
#1
of 1 outputs
Altmetric has tracked 25,988,468 research outputs across all sources so far. This one is in the 10th percentile – i.e., 10% of other outputs scored the same or lower than it.
So far Altmetric has tracked 410 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.9. This one is in the 4th percentile – i.e., 4% 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 339,111 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 11th percentile – i.e., 11% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 1 others from the same source and published within six weeks on either side of this one. This one has scored higher than all of them