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Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms
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| Zeitschriftentitel: | Chemical Biology & Drug Design |
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| Personen und Körperschaften: | , , , , , |
| In: | Chemical Biology & Drug Design, 91, 2018, 1, S. 332-337 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
Wiley
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| Schlagwörter: |
| author_facet |
Jordan, Brian C. Kumar, Bhavna Thilagavathi, Ramasamy Yadhav, Arti Kumar, Pawan Selvam, Chelliah Jordan, Brian C. Kumar, Bhavna Thilagavathi, Ramasamy Yadhav, Arti Kumar, Pawan Selvam, Chelliah |
|---|---|
| author |
Jordan, Brian C. Kumar, Bhavna Thilagavathi, Ramasamy Yadhav, Arti Kumar, Pawan Selvam, Chelliah |
| spellingShingle |
Jordan, Brian C. Kumar, Bhavna Thilagavathi, Ramasamy Yadhav, Arti Kumar, Pawan Selvam, Chelliah Chemical Biology & Drug Design Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry |
| author_sort |
jordan, brian c. |
| spelling |
Jordan, Brian C. Kumar, Bhavna Thilagavathi, Ramasamy Yadhav, Arti Kumar, Pawan Selvam, Chelliah 1747-0277 1747-0285 Wiley Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry http://dx.doi.org/10.1111/cbdd.13061 <jats:p>Curcumin is a popular, plant‐derived compound that has been extensively investigated for diverse range of biological activities. Anticancer activity against various types of cancers and high‐safety profile associated with curcumin makes it very attractive. In this study, we report the synthesis and evaluation of pyrazole and click chemistry curcumin analogues for Head and Neck cancer. <jats:styled-content style="fixed-case">MTT</jats:styled-content> assay against head and neck cancer cell lines <jats:styled-content style="fixed-case">CAL</jats:styled-content>27 and <jats:styled-content style="fixed-case">UM</jats:styled-content>‐<jats:styled-content style="fixed-case">SCC</jats:styled-content>‐74A revealed the micromolar potency of the synthesized compounds. To determine the possible molecular mechanisms, effect of these analogues in the expression of <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3, <jats:styled-content style="fixed-case">pFAK</jats:styled-content>,<jats:styled-content style="fixed-case"> pERK</jats:styled-content>1/2 and <jats:styled-content style="fixed-case">pAKT</jats:styled-content> was studied. Interestingly, compounds <jats:bold>2</jats:bold> and <jats:bold>5</jats:bold> significantly inhibited the <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 (Tyr 705) phosphorylation. As far as other compounds, they showed potent cytotoxicity against <jats:styled-content style="fixed-case">CAL</jats:styled-content>27; however, these compounds did not show any activity on <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 phosphorylation at <jats:styled-content style="fixed-case">IC</jats:styled-content><jats:sub>50</jats:sub> concentration level. Molecular docking studies revealed the possible binding mode of pyrazole compound <jats:bold>2</jats:bold> in the <jats:styled-content style="fixed-case">SH</jats:styled-content>2 domain of STAT3.</jats:p> Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms Chemical Biology & Drug Design |
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| title |
Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_unstemmed |
Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_full |
Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_fullStr |
Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_full_unstemmed |
Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_short |
Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_sort |
synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| topic |
Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry |
| url |
http://dx.doi.org/10.1111/cbdd.13061 |
| publishDate |
2018 |
| physical |
332-337 |
| description |
<jats:p>Curcumin is a popular, plant‐derived compound that has been extensively investigated for diverse range of biological activities. Anticancer activity against various types of cancers and high‐safety profile associated with curcumin makes it very attractive. In this study, we report the synthesis and evaluation of pyrazole and click chemistry curcumin analogues for Head and Neck cancer. <jats:styled-content style="fixed-case">MTT</jats:styled-content> assay against head and neck cancer cell lines <jats:styled-content style="fixed-case">CAL</jats:styled-content>27 and <jats:styled-content style="fixed-case">UM</jats:styled-content>‐<jats:styled-content style="fixed-case">SCC</jats:styled-content>‐74A revealed the micromolar potency of the synthesized compounds. To determine the possible molecular mechanisms, effect of these analogues in the expression of <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3, <jats:styled-content style="fixed-case">pFAK</jats:styled-content>,<jats:styled-content style="fixed-case"> pERK</jats:styled-content>1/2 and <jats:styled-content style="fixed-case">pAKT</jats:styled-content> was studied. Interestingly, compounds <jats:bold>2</jats:bold> and <jats:bold>5</jats:bold> significantly inhibited the <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 (Tyr 705) phosphorylation. As far as other compounds, they showed potent cytotoxicity against <jats:styled-content style="fixed-case">CAL</jats:styled-content>27; however, these compounds did not show any activity on <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 phosphorylation at <jats:styled-content style="fixed-case">IC</jats:styled-content><jats:sub>50</jats:sub> concentration level. Molecular docking studies revealed the possible binding mode of pyrazole compound <jats:bold>2</jats:bold> in the <jats:styled-content style="fixed-case">SH</jats:styled-content>2 domain of STAT3.</jats:p> |
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| author | Jordan, Brian C., Kumar, Bhavna, Thilagavathi, Ramasamy, Yadhav, Arti, Kumar, Pawan, Selvam, Chelliah |
| author_facet | Jordan, Brian C., Kumar, Bhavna, Thilagavathi, Ramasamy, Yadhav, Arti, Kumar, Pawan, Selvam, Chelliah, Jordan, Brian C., Kumar, Bhavna, Thilagavathi, Ramasamy, Yadhav, Arti, Kumar, Pawan, Selvam, Chelliah |
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| description | <jats:p>Curcumin is a popular, plant‐derived compound that has been extensively investigated for diverse range of biological activities. Anticancer activity against various types of cancers and high‐safety profile associated with curcumin makes it very attractive. In this study, we report the synthesis and evaluation of pyrazole and click chemistry curcumin analogues for Head and Neck cancer. <jats:styled-content style="fixed-case">MTT</jats:styled-content> assay against head and neck cancer cell lines <jats:styled-content style="fixed-case">CAL</jats:styled-content>27 and <jats:styled-content style="fixed-case">UM</jats:styled-content>‐<jats:styled-content style="fixed-case">SCC</jats:styled-content>‐74A revealed the micromolar potency of the synthesized compounds. To determine the possible molecular mechanisms, effect of these analogues in the expression of <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3, <jats:styled-content style="fixed-case">pFAK</jats:styled-content>,<jats:styled-content style="fixed-case"> pERK</jats:styled-content>1/2 and <jats:styled-content style="fixed-case">pAKT</jats:styled-content> was studied. Interestingly, compounds <jats:bold>2</jats:bold> and <jats:bold>5</jats:bold> significantly inhibited the <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 (Tyr 705) phosphorylation. As far as other compounds, they showed potent cytotoxicity against <jats:styled-content style="fixed-case">CAL</jats:styled-content>27; however, these compounds did not show any activity on <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 phosphorylation at <jats:styled-content style="fixed-case">IC</jats:styled-content><jats:sub>50</jats:sub> concentration level. Molecular docking studies revealed the possible binding mode of pyrazole compound <jats:bold>2</jats:bold> in the <jats:styled-content style="fixed-case">SH</jats:styled-content>2 domain of STAT3.</jats:p> |
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| spelling | Jordan, Brian C. Kumar, Bhavna Thilagavathi, Ramasamy Yadhav, Arti Kumar, Pawan Selvam, Chelliah 1747-0277 1747-0285 Wiley Molecular Medicine Biochemistry Drug Discovery Pharmacology Organic Chemistry http://dx.doi.org/10.1111/cbdd.13061 <jats:p>Curcumin is a popular, plant‐derived compound that has been extensively investigated for diverse range of biological activities. Anticancer activity against various types of cancers and high‐safety profile associated with curcumin makes it very attractive. In this study, we report the synthesis and evaluation of pyrazole and click chemistry curcumin analogues for Head and Neck cancer. <jats:styled-content style="fixed-case">MTT</jats:styled-content> assay against head and neck cancer cell lines <jats:styled-content style="fixed-case">CAL</jats:styled-content>27 and <jats:styled-content style="fixed-case">UM</jats:styled-content>‐<jats:styled-content style="fixed-case">SCC</jats:styled-content>‐74A revealed the micromolar potency of the synthesized compounds. To determine the possible molecular mechanisms, effect of these analogues in the expression of <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3, <jats:styled-content style="fixed-case">pFAK</jats:styled-content>,<jats:styled-content style="fixed-case"> pERK</jats:styled-content>1/2 and <jats:styled-content style="fixed-case">pAKT</jats:styled-content> was studied. Interestingly, compounds <jats:bold>2</jats:bold> and <jats:bold>5</jats:bold> significantly inhibited the <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 (Tyr 705) phosphorylation. As far as other compounds, they showed potent cytotoxicity against <jats:styled-content style="fixed-case">CAL</jats:styled-content>27; however, these compounds did not show any activity on <jats:styled-content style="fixed-case">pSTAT</jats:styled-content>3 phosphorylation at <jats:styled-content style="fixed-case">IC</jats:styled-content><jats:sub>50</jats:sub> concentration level. Molecular docking studies revealed the possible binding mode of pyrazole compound <jats:bold>2</jats:bold> in the <jats:styled-content style="fixed-case">SH</jats:styled-content>2 domain of STAT3.</jats:p> Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms Chemical Biology & Drug Design |
| spellingShingle | Jordan, Brian C., Kumar, Bhavna, Thilagavathi, Ramasamy, Yadhav, Arti, Kumar, Pawan, Selvam, Chelliah, Chemical Biology & Drug Design, Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms, Molecular Medicine, Biochemistry, Drug Discovery, Pharmacology, Organic Chemistry |
| title | Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_full | Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_fullStr | Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_full_unstemmed | Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_short | Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_sort | synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| title_unstemmed | Synthesis, evaluation of cytotoxic properties of promising curcumin analogues and investigation of possible molecular mechanisms |
| topic | Molecular Medicine, Biochemistry, Drug Discovery, Pharmacology, Organic Chemistry |
| url | http://dx.doi.org/10.1111/cbdd.13061 |