Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold
A bisamide compound 1 possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and biologically evaluated. It was tested for kinase inhibitory activity over a panel of 47 kinases, and its selectivity toward the FMS kinase was accidentally discovered. Compound 1 was tested over a panel of seven...
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| Veröffentlicht in: | Archiv der Pharmazie (Weinheim) 2014-09, Vol.347 (9), p.635-641 |
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| container_title | Archiv der Pharmazie (Weinheim) |
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| creator | El-Gamal, Mohammed I. Abdel-Maksoud, Mohammed S. El-Din, Mahmoud M. Gamal Yoo, Kyung Ho Baek, Daejin Oh, Chang-Hyun |
| description | A bisamide compound 1 possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and biologically evaluated. It was tested for kinase inhibitory activity over a panel of 47 kinases, and its selectivity toward the FMS kinase was accidentally discovered. Compound 1 was tested over a panel of seven ovarian, two prostate, and six breast cancer cell lines at a single dose concentration of 10 µM and showed high activity. It was further tested in a 5‐dose mode to determine its IC50 and total growth inhibition (TGI) values over the 15 cell lines. Compound 1 showed high potency on the submicromolar scale and good efficacy. The cytotoxic effect of compound 1 over peritoneal macrophages was also investigated. Compound 1 demonstrated higher selectivity against different cancer cell lines compared with HS‐27 fibroblasts.
A bisamide compound (1) possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and evaluated as kinase inhibitor, by screening a panel of 47 kinases. Compound 1 was found to possess selectivity for the FMS kinase, with inhibitory activity on the submicromolar scale. The cytotoxic effect of compound 1 was investigated on 15 cancer cell lines and on peritoneal macrophages. |
| doi_str_mv | 10.1002/ardp.201400051 |
| format | Article |
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A bisamide compound (1) possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and evaluated as kinase inhibitor, by screening a panel of 47 kinases. Compound 1 was found to possess selectivity for the FMS kinase, with inhibitory activity on the submicromolar scale. The cytotoxic effect of compound 1 was investigated on 15 cancer cell lines and on peritoneal macrophages.</description><identifier>ISSN: 0365-6233</identifier><identifier>EISSN: 1521-4184</identifier><identifier>DOI: 10.1002/ardp.201400051</identifier><identifier>PMID: 24942978</identifier><language>eng</language><publisher>Germany: Blackwell Publishing Ltd</publisher><subject>2-c]pyridine ; Amides - chemical synthesis ; Amides - chemistry ; Amides - pharmacology ; Anticancer ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Bisamide ; Cell Line, Tumor ; Cell Proliferation - drug effects ; Cell Survival - drug effects ; Diarylamide ; Dose-Response Relationship, Drug ; Fibroblasts - drug effects ; FMS kinase ; Humans ; Inhibitory Concentration 50 ; Macrophages, Peritoneal - drug effects ; Protein Kinase Inhibitors - chemical synthesis ; Protein Kinase Inhibitors - chemistry ; Protein Kinase Inhibitors - pharmacokinetics ; Pyridines - chemistry ; Pyrroles - chemistry ; Pyrrolo ; Pyrrolo[3,2‐c]pyridine ; Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors</subject><ispartof>Archiv der Pharmazie (Weinheim), 2014-09, Vol.347 (9), p.635-641</ispartof><rights>2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim</rights><rights>2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4811-a8b503341dc440e12e790e9ff3858ab299170fe99080c4691f1bb99a89dc2c7b3</citedby><cites>FETCH-LOGICAL-c4811-a8b503341dc440e12e790e9ff3858ab299170fe99080c4691f1bb99a89dc2c7b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fardp.201400051$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fardp.201400051$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/24942978$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>El-Gamal, Mohammed I.</creatorcontrib><creatorcontrib>Abdel-Maksoud, Mohammed S.</creatorcontrib><creatorcontrib>El-Din, Mahmoud M. Gamal</creatorcontrib><creatorcontrib>Yoo, Kyung Ho</creatorcontrib><creatorcontrib>Baek, Daejin</creatorcontrib><creatorcontrib>Oh, Chang-Hyun</creatorcontrib><title>Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold</title><title>Archiv der Pharmazie (Weinheim)</title><addtitle>Arch. Pharm. Chem. Life Sci</addtitle><description>A bisamide compound 1 possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and biologically evaluated. It was tested for kinase inhibitory activity over a panel of 47 kinases, and its selectivity toward the FMS kinase was accidentally discovered. Compound 1 was tested over a panel of seven ovarian, two prostate, and six breast cancer cell lines at a single dose concentration of 10 µM and showed high activity. It was further tested in a 5‐dose mode to determine its IC50 and total growth inhibition (TGI) values over the 15 cell lines. Compound 1 showed high potency on the submicromolar scale and good efficacy. The cytotoxic effect of compound 1 over peritoneal macrophages was also investigated. Compound 1 demonstrated higher selectivity against different cancer cell lines compared with HS‐27 fibroblasts.
A bisamide compound (1) possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and evaluated as kinase inhibitor, by screening a panel of 47 kinases. Compound 1 was found to possess selectivity for the FMS kinase, with inhibitory activity on the submicromolar scale. The cytotoxic effect of compound 1 was investigated on 15 cancer cell lines and on peritoneal macrophages.</description><subject>2-c]pyridine</subject><subject>Amides - chemical synthesis</subject><subject>Amides - chemistry</subject><subject>Amides - pharmacology</subject><subject>Anticancer</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Bisamide</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Cell Survival - drug effects</subject><subject>Diarylamide</subject><subject>Dose-Response Relationship, Drug</subject><subject>Fibroblasts - drug effects</subject><subject>FMS kinase</subject><subject>Humans</subject><subject>Inhibitory Concentration 50</subject><subject>Macrophages, Peritoneal - drug effects</subject><subject>Protein Kinase Inhibitors - chemical synthesis</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - pharmacokinetics</subject><subject>Pyridines - chemistry</subject><subject>Pyrroles - chemistry</subject><subject>Pyrrolo</subject><subject>Pyrrolo[3,2‐c]pyridine</subject><subject>Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors</subject><issn>0365-6233</issn><issn>1521-4184</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2014</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1vEzEURS0EoqGwZYkssWHBhOevGXvZhrYU2hLRoC4Qsjweu7hMxsHOUPLvcZUSITas3sLnHr3ni9BzAlMCQN-Y1K2mFAgHAEEeoAkRlFScSP4QTYDVoqopY3voSc43BWFAxWO0R7niVDVygtLM9X11aLLr8GGIfbwO1vT46KfpR7MOccDRY4Mv3G15zmYZOoePzy_xhzCUDD4dvoU2rGPC85izyzkM13i-SamYvrDXtLJfV5sUujA4fGmN97HvnqJH3vTZPbuf--jz8dFi9q46-3hyOjs4qyyXhFRGtgIY46SznIMj1DUKnPKeSSFNS5UiDXinFEiwvFbEk7ZVykjVWWqblu2jV1vvKsUfo8trvQzZlnPN4OKYNRFCASgh6oK-_Ae9iWMaynaFqimpRQ2iUNMtZVM5NjmvVyksTdpoAvquDX3Xht61UQIv7rVju3TdDv_z_QVQW-A29G7zH50--PR2_re82mZDXrtfu6xJ33XdsEboq4sTreZXs3P5fqEX7Df2zqQk</recordid><startdate>201409</startdate><enddate>201409</enddate><creator>El-Gamal, Mohammed I.</creator><creator>Abdel-Maksoud, Mohammed S.</creator><creator>El-Din, Mahmoud M. Gamal</creator><creator>Yoo, Kyung Ho</creator><creator>Baek, Daejin</creator><creator>Oh, Chang-Hyun</creator><general>Blackwell Publishing Ltd</general><general>Wiley Subscription Services, Inc</general><scope>BSCLL</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>K9.</scope><scope>7X8</scope></search><sort><creationdate>201409</creationdate><title>Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold</title><author>El-Gamal, Mohammed I. ; Abdel-Maksoud, Mohammed S. ; El-Din, Mahmoud M. Gamal ; Yoo, Kyung Ho ; Baek, Daejin ; Oh, Chang-Hyun</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4811-a8b503341dc440e12e790e9ff3858ab299170fe99080c4691f1bb99a89dc2c7b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2014</creationdate><topic>2-c]pyridine</topic><topic>Amides - chemical synthesis</topic><topic>Amides - chemistry</topic><topic>Amides - pharmacology</topic><topic>Anticancer</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Bisamide</topic><topic>Cell Line, Tumor</topic><topic>Cell Proliferation - drug effects</topic><topic>Cell Survival - drug effects</topic><topic>Diarylamide</topic><topic>Dose-Response Relationship, Drug</topic><topic>Fibroblasts - drug effects</topic><topic>FMS kinase</topic><topic>Humans</topic><topic>Inhibitory Concentration 50</topic><topic>Macrophages, Peritoneal - drug effects</topic><topic>Protein Kinase Inhibitors - chemical synthesis</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Protein Kinase Inhibitors - pharmacokinetics</topic><topic>Pyridines - chemistry</topic><topic>Pyrroles - chemistry</topic><topic>Pyrrolo</topic><topic>Pyrrolo[3,2‐c]pyridine</topic><topic>Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>El-Gamal, Mohammed I.</creatorcontrib><creatorcontrib>Abdel-Maksoud, Mohammed S.</creatorcontrib><creatorcontrib>El-Din, Mahmoud M. Gamal</creatorcontrib><creatorcontrib>Yoo, Kyung Ho</creatorcontrib><creatorcontrib>Baek, Daejin</creatorcontrib><creatorcontrib>Oh, Chang-Hyun</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>MEDLINE - Academic</collection><jtitle>Archiv der Pharmazie (Weinheim)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>El-Gamal, Mohammed I.</au><au>Abdel-Maksoud, Mohammed S.</au><au>El-Din, Mahmoud M. Gamal</au><au>Yoo, Kyung Ho</au><au>Baek, Daejin</au><au>Oh, Chang-Hyun</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold</atitle><jtitle>Archiv der Pharmazie (Weinheim)</jtitle><addtitle>Arch. Pharm. Chem. Life Sci</addtitle><date>2014-09</date><risdate>2014</risdate><volume>347</volume><issue>9</issue><spage>635</spage><epage>641</epage><pages>635-641</pages><issn>0365-6233</issn><eissn>1521-4184</eissn><abstract>A bisamide compound 1 possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and biologically evaluated. It was tested for kinase inhibitory activity over a panel of 47 kinases, and its selectivity toward the FMS kinase was accidentally discovered. Compound 1 was tested over a panel of seven ovarian, two prostate, and six breast cancer cell lines at a single dose concentration of 10 µM and showed high activity. It was further tested in a 5‐dose mode to determine its IC50 and total growth inhibition (TGI) values over the 15 cell lines. Compound 1 showed high potency on the submicromolar scale and good efficacy. The cytotoxic effect of compound 1 over peritoneal macrophages was also investigated. Compound 1 demonstrated higher selectivity against different cancer cell lines compared with HS‐27 fibroblasts.
A bisamide compound (1) possessing the pyrrolo[3,2‐c]pyridine nucleus was synthesized and evaluated as kinase inhibitor, by screening a panel of 47 kinases. Compound 1 was found to possess selectivity for the FMS kinase, with inhibitory activity on the submicromolar scale. The cytotoxic effect of compound 1 was investigated on 15 cancer cell lines and on peritoneal macrophages.</abstract><cop>Germany</cop><pub>Blackwell Publishing Ltd</pub><pmid>24942978</pmid><doi>10.1002/ardp.201400051</doi><tpages>7</tpages></addata></record> |
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| ispartof | Archiv der Pharmazie (Weinheim), 2014-09, Vol.347 (9), p.635-641 |
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| language | eng |
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| subjects | 2-c]pyridine Amides - chemical synthesis Amides - chemistry Amides - pharmacology Anticancer Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Bisamide Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects Diarylamide Dose-Response Relationship, Drug Fibroblasts - drug effects FMS kinase Humans Inhibitory Concentration 50 Macrophages, Peritoneal - drug effects Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacokinetics Pyridines - chemistry Pyrroles - chemistry Pyrrolo Pyrrolo[3,2‐c]pyridine Receptor, Macrophage Colony-Stimulating Factor - antagonists & inhibitors |
| title | Cell-Based Biological Evaluation of a New Bisamide FMS Kinase Inhibitor Possessing Pyrrolo[3,2-c]pyridine Scaffold |
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