Synthesis, Characterisation, and In Vitro Anticancer Activity of Curcumin Analogues Bearing Pyrazole/Pyrimidine Ring Targeting EGFR Tyrosine Kinase

In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening...

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Published inBioMed research international Vol. 2013; no. 2013; pp. 1 - 14
Main Authors Jadav, Surender Singh, Yasmin, Sabina, Khalilullah, Habibullah, Ahsan, Mohamed Jawed, Govindasamy, Jeyabalan
Format Journal Article
LanguageEnglish
Published Cairo, Egypt Hindawi Publishing Corporation 01.01.2013
Hindawi Limited
Subjects
Binding Sites - drug effects
Cancer
Cancer therapies
Cell Line, Tumor - drug effects
Crystallography, X-Ray
Curcumin - administration & dosage
Curcumin - analogs & derivatives
Curcumin - chemical synthesis
Cytotoxicity
Humans
Hydrogen bonds
Kinases
Ligands
Molecular Docking Simulation
Pharmaceuticals
Protein Kinase Inhibitors - administration & dosage
Protein Kinase Inhibitors - chemical synthesis
Pyrazoles - administration & dosage
Pyrazoles - chemical synthesis
Pyrimidines - administration & dosage
Pyrimidines - chemical synthesis
Receptor, Epidermal Growth Factor - antagonists & inhibitors
Receptor, Epidermal Growth Factor - chemistry
Receptor, Epidermal Growth Factor - metabolism
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Abstract In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H-pyrazole-1-yl(phenyl)methanone (10) which showed mean growth percent of −28.71 in one-dose assay and GI50 values between 0.0079 and 1.86 µM in 5-dose assay.
AbstractList In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H-pyrazole-1-yl(phenyl)methanone (10) which showed mean growth percent of -28.71 in one-dose assay and GI50 values between 0.0079 and 1.86 µM in 5-dose assay.
In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1 H -pyrazole-1-yl(phenyl)methanone ( 10 ) which showed mean growth percent of −28.71 in one-dose assay and GI 50 values between 0.0079 and 1.86 µM in 5-dose assay.
In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H-pyrazole-1-yl(phenyl)methanone which showed mean growth percent of -28.71 in one-dose assay and GI₅₀ values between 0.0079 and 1.86 µM in 5-dose assay.
In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H-pyrazole-1-yl(phenyl)methanone (10) which showed mean growth percent of −28.71 in one-dose assay and GI50 values between 0.0079 and 1.86 µM in 5-dose assay.
In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1H -pyrazole-1-yl(phenyl)methanone (10 ) which showed mean growth percent of -28.71 in one-dose assay and GI sub(50) values between 0.0079 and 1.86 mu M in 5-dose assay.
In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of curcumin analogues. The anticancer effects were evaluated on a panel of 60 cell lines, according to the National Cancer Institute (NCI) screening protocol. There were 10 tested compounds among 14 synthesized compounds, which showed potent anticancer activity in both one-dose and 5-dose assays. The most active compound of the series was 3,5-bis(4-hydroxy-3-methylstyryl)-1 H -pyrazole-1-yl(phenyl)methanone ( 10 ) which showed mean growth percent of −28.71 in one-dose assay and GI 50 values between 0.0079 and 1.86  µ M in 5-dose assay.
Author Jadav, Surender Singh
Ahsan, Mohamed Jawed
Yasmin, Sabina
Khalilullah, Habibullah
Govindasamy, Jeyabalan
AuthorAffiliation 1 Department of Pharmaceutical Chemistry, Maharishi Arvind College of Pharmacy, Ambabari, Jaipur, Rajasthan 302 023, India
2 Department of Pharmaceutical Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301 030, India
3 Department of Pharmaceutical Chemistry, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835 215, India
AuthorAffiliation_xml – name: 1 Department of Pharmaceutical Chemistry, Maharishi Arvind College of Pharmacy, Ambabari, Jaipur, Rajasthan 302 023, India
– name: 3 Department of Pharmaceutical Chemistry, Birla Institute of Technology, Mesra, Ranchi, Jharkhand 835 215, India
– name: 2 Department of Pharmaceutical Chemistry, Alwar Pharmacy College, Alwar, Rajasthan 301 030, India
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  fullname: Khalilullah, Habibullah
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/24089667$$D View this record in MEDLINE/PubMed
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ContentType Journal Article
Copyright Copyright © 2013 Mohamed Jawed Ahsan et al.
Copyright © 2013 Mohamed Jawed Ahsan et al. Mohamed Jawed Ahsan et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Copyright © 2013 Mohamed Jawed Ahsan et al. 2013
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Snippet In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of...
In search of potential therapeutics for cancer, we described herein the synthesis, characterization, and in vitro anticancer activity of a novel series of...
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StartPage 1
SubjectTerms Binding Sites - drug effects
Cancer
Cancer therapies
Cell Line, Tumor - drug effects
Crystallography, X-Ray
Curcumin - administration & dosage
Curcumin - analogs & derivatives
Curcumin - chemical synthesis
Cytotoxicity
Humans
Hydrogen bonds
Kinases
Ligands
Molecular Docking Simulation
Pharmaceuticals
Protein Kinase Inhibitors - administration & dosage
Protein Kinase Inhibitors - chemical synthesis
Pyrazoles - administration & dosage
Pyrazoles - chemical synthesis
Pyrimidines - administration & dosage
Pyrimidines - chemical synthesis
Receptor, Epidermal Growth Factor - antagonists & inhibitors
Receptor, Epidermal Growth Factor - chemistry
Receptor, Epidermal Growth Factor - metabolism
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Title Synthesis, Characterisation, and In Vitro Anticancer Activity of Curcumin Analogues Bearing Pyrazole/Pyrimidine Ring Targeting EGFR Tyrosine Kinase
URI https://search.emarefa.net/detail/BIM-1030215
https://dx.doi.org/10.1155/2013/239354
https://www.ncbi.nlm.nih.gov/pubmed/24089667
https://www.proquest.com/docview/1444522475/abstract/
https://search.proquest.com/docview/1443396886
https://search.proquest.com/docview/1508758182
https://pubmed.ncbi.nlm.nih.gov/PMC3781846
Volume 2013
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