A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity
A novel 2-(furan-2-yl)-4-(pyridin-2-yl)-5H-indeno[1,2-b]pyridin-5-one (TI-1-190) was synthesized using a simple microwave-assisted method and its mode of action was systematically characterized. It is a DNA intercalative human topoisomerase IIα catalytic inhibitor with much stronger activity and les...
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| Veröffentlicht in: | Chemical communications (Cambridge, England) England), 2017-06, Vol.53 (51), p.6864-6867 |
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| container_issue | 51 |
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| container_title | Chemical communications (Cambridge, England) |
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| creator | Jeon, K H Park, C Kadayat, T M Shrestha, A Lee, E S Kwon, Y |
| description | A novel 2-(furan-2-yl)-4-(pyridin-2-yl)-5H-indeno[1,2-b]pyridin-5-one (TI-1-190) was synthesized using a simple microwave-assisted method and its mode of action was systematically characterized. It is a DNA intercalative human topoisomerase IIα catalytic inhibitor with much stronger activity and less DNA toxicity than etoposide, a topoisomerase II poison. TI-1-190 displays caspase 3-independent anticancer activity, unlike etoposide. |
| doi_str_mv | 10.1039/c7cc02372c |
| format | Article |
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TI-1-190 displays caspase 3-independent anticancer activity, unlike etoposide.</description><subject>Anticancer properties</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Apoptosis - drug effects</subject><subject>Biocatalysis</subject><subject>Biocompatibility</subject><subject>Caspase 3 - metabolism</subject><subject>Catalysis</subject><subject>Catalysts</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Deoxyribonucleic acid</subject><subject>Derivatives</subject><subject>DNA Topoisomerases, Type II - metabolism</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Humans</subject><subject>Inhibitors</subject><subject>Intercalating Agents - chemical synthesis</subject><subject>Intercalating Agents - chemistry</subject><subject>Intercalating Agents - pharmacology</subject><subject>MCF-7 Cells</subject><subject>Molecular Structure</subject><subject>Poly-ADP-Ribose Binding Proteins - antagonists & inhibitors</subject><subject>Poly-ADP-Ribose Binding Proteins - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Surgical implants</subject><subject>Topoisomerase II Inhibitors - chemical synthesis</subject><subject>Topoisomerase II Inhibitors - chemistry</subject><subject>Topoisomerase II Inhibitors - pharmacology</subject><issn>1359-7345</issn><issn>1364-548X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkU2O1DAQhS0EYn5gwwGQlwh1wI7j2Fm2wgy0NJrZgISEUOSfisYosYPtbqnPwim4yJwJZ2ZgTW2qVPXVe4uH0CtK3lHCuvdGGENqJmrzBJ1S1jYVb-TXp-vMu0qwhp-gs5R-kFKUy-fopJYtaSSvT9GvLfbhABN23oIP3-imrvT35RiddT54wBaiO6jsDrDBCn-43hYyQzRqul_i2_2sPM5hCS6FGaJKgHe7u9_YqKymY3amPNw67XKIGzyGWA5pWSlWrZ4LrMYZK19Q5Q1ErExRdvn4Aj0b1ZTg5WM_R18uLz73n6qrm4-7fntVGcZZrmQridbG2pYJIcrcidbKjlo-CqvFSIS0pqWd5sYq2hBrWQuK2EYTqqUl7By9edBdYvi5h5SH2SUD06Q8hH0aaFdzKbqatv-BFkh0pOYFffuAmhhSijAOS3SziseBkmHNbehF39_n1hf49aPuXs9g_6F_g2J_AD3-lgs</recordid><startdate>20170622</startdate><enddate>20170622</enddate><creator>Jeon, K H</creator><creator>Park, C</creator><creator>Kadayat, T M</creator><creator>Shrestha, A</creator><creator>Lee, E S</creator><creator>Kwon, Y</creator><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>7TM</scope><scope>7SR</scope><scope>7U5</scope><scope>8BQ</scope><scope>8FD</scope><scope>JG9</scope><scope>L7M</scope><orcidid>https://orcid.org/0000-0001-6256-3042</orcidid></search><sort><creationdate>20170622</creationdate><title>A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity</title><author>Jeon, K H ; 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| source | MEDLINE; Royal Society Of Chemistry Journals 2008-; Alma/SFX Local Collection |
| subjects | Anticancer properties Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis - drug effects Biocatalysis Biocompatibility Caspase 3 - metabolism Catalysis Catalysts Cell Line, Tumor Cell Proliferation - drug effects Deoxyribonucleic acid Derivatives DNA Topoisomerases, Type II - metabolism Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Inhibitors Intercalating Agents - chemical synthesis Intercalating Agents - chemistry Intercalating Agents - pharmacology MCF-7 Cells Molecular Structure Poly-ADP-Ribose Binding Proteins - antagonists & inhibitors Poly-ADP-Ribose Binding Proteins - metabolism Structure-Activity Relationship Surgical implants Topoisomerase II Inhibitors - chemical synthesis Topoisomerase II Inhibitors - chemistry Topoisomerase II Inhibitors - pharmacology |
| title | A novel indeno[1,2-b]pyridinone derivative, a DNA intercalative human topoisomerase IIα catalytic inhibitor, for caspase 3-independent anticancer activity |
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