2019
DOI: 10.1016/j.ejmech.2018.12.011
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Design, synthesis, in silico pharmacokinetics prediction and biological evaluation of 1,4-dihydroindeno[1,2-c]pyrazole chalcone as EGFR /Akt pathway inhibitors

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Cited by 46 publications
(21 citation statements)
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“…A series of 7-amino- [1,2,4] triazolo [4,3-f] pteridinone, and 7-aminotetrazolo[1,5-f] pteridinone derivative (35 compounds) as NSCLC therapeutic agents were sourced from the literature and used in this work [15]. After the dataset were sourced, Chemdraw software version 12.0.1 was used to achieve the sketching of the 2D structures of all the dataset under consideration [16].…”
Section: Sourcing Sketching and Determination Of The Optimum Structumentioning
confidence: 99%
See 1 more Smart Citation
“…A series of 7-amino- [1,2,4] triazolo [4,3-f] pteridinone, and 7-aminotetrazolo[1,5-f] pteridinone derivative (35 compounds) as NSCLC therapeutic agents were sourced from the literature and used in this work [15]. After the dataset were sourced, Chemdraw software version 12.0.1 was used to achieve the sketching of the 2D structures of all the dataset under consideration [16].…”
Section: Sourcing Sketching and Determination Of The Optimum Structumentioning
confidence: 99%
“…Cancer was recognised to be daunting illness and second cause of death globally. The death estimate caused by cancer as of 2012 was about 17% of the total deaths (which is about 8.5 million) and in 2030 will be about 13.1 million deaths [1]. Lung cancer is one of the leading cancer problems in the globe.…”
Section: Introductionmentioning
confidence: 99%
“…Synthetic accessibility score of all the compounds under investigation including the three (3) hit compounds was less than 5 showing that they can be easily synthesized in the laboratory. The compounds under investigation including the three hit compounds were predicted to have good pharmacokinetic profile and drug-likeness except compound 16 [24,25].…”
Section: Drug-likeness and Adme Property Prediction Of The Studied Comentioning
confidence: 99%
“…None of the designed compounds was found to violate more than two of the permissible limit set by the Lipinski's rule of five filters for small molecules. Based on that, their permeability across the cell membrane, easy transportation, absorption, and diffusion was predicted [24,26].…”
Section: Drug-likeness and Adme Prediction Of The Newly Designed Compmentioning
confidence: 99%
“…It also exhibited a very broad range of beneficial biological activities including antimicrobial (antibacterial, antifungal), anti‐inflammatory, anti‐parasitic (anti‐malarial, anti‐leishmanial), antioxidant, antimitotic, anti‐invasive, anti‐tuberculosis, anticancer, as well as modulation of P‐glycoprotein‐mediated multidrug resistance . Chalcones are regarded as promising anticancer agents by interacting with cellular targets like Nrf2/ARE, EGFR, ODC, proteasome, nuclear factor‐κB (NF‐κB)‐mediated defense mechanisms and also by its strong capability of inducing apoptosis . Similarly, it may be lacking important genotoxic side effects like amino group interaction of nucleic acids which was exhibited by a number of clinically useful anticancer drugs.…”
Section: Introductionmentioning
confidence: 99%