Comparative in vitro studies of tiazofurin and a selenazole analog
2-β-D-Ribofuranosylselenazole-4-carboxamide, a selenazole analog of the antitumor agent Tiazofurin, is severalfold more cytotoxic to murine tumor cells in culture than Tiazofurin. Like Tiazofurin, the cytotoxicity of the selenazole analog is reversed by exogenous guanosine, and both nucleosides spec...
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| Veröffentlicht in: | Biochemical and biophysical research communications 1983-09, Vol.115 (2), p.544-550 |
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| container_title | Biochemical and biophysical research communications |
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| creator | Streeter, David G. Robins, Roland K. |
| description | 2-β-D-Ribofuranosylselenazole-4-carboxamide, a selenazole analog of the antitumor agent Tiazofurin, is severalfold more cytotoxic to murine tumor cells in culture than Tiazofurin. Like Tiazofurin, the cytotoxicity of the selenazole analog is reversed by exogenous guanosine, and both nucleosides specifically inhibit IMP dehydrogenase activity in cultured P388 cells. The dose-dependency for this inhibition correlates with the relative cytotoxicities of both drugs, indicating that a more potent inhibition of IMP dehydrogenase by the selenazole analog is primarily responsible for its increased cytotoxicity. The specific inhibition of the isolated enzyme by potential metabolites of the selenazole analog is discussed. |
| doi_str_mv | 10.1016/S0006-291X(83)80179-X |
| format | Article |
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The specific inhibition of the isolated enzyme by potential metabolites of the selenazole analog is discussed.</description><subject>Animals</subject><subject>Antineoplastic Agents</subject><subject>Cell Survival - drug effects</subject><subject>IMP Dehydrogenase - metabolism</subject><subject>Leukemia L1210 - drug therapy</subject><subject>Leukemia L1210 - enzymology</subject><subject>Leukemia P388 - drug therapy</subject><subject>Leukemia P388 - enzymology</subject><subject>Leukemia, Experimental - drug therapy</subject><subject>Mice</subject><subject>Nucleoside-Diphosphate Kinase - antagonists & inhibitors</subject><subject>Organoselenium Compounds</subject><subject>Ribavirin - analogs & derivatives</subject><subject>Ribavirin - therapeutic use</subject><subject>Ribonucleosides - therapeutic use</subject><subject>Selenium - therapeutic use</subject><issn>0006-291X</issn><issn>1090-2104</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1983</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kE1LxDAQhoMo67r6ExZ6Ej1UJ02aJifRxS9Y8KDC3kLaTiXSNmuSLuivt-4ungbe92GYeQiZU7iiQMX1KwCINFN0dSHZpQRaqHR1QKYUFKQZBX5Ipv_IMTkJ4ROAUi7UhEwEZRKYmJK7hevWxptoN5jYPtnY6F0S4lBbDIlrkmjNj2sGP3amrxOTBGyxH7MWx8C07uOUHDWmDXi2nzPy_nD_tnhKly-Pz4vbZYq0KGJaGcWA80xIJQAYLZnkZZ4j5EVVNbRmWQmNFIznHJuylCyTyFVmmMmZKaRhM3K-27v27mvAEHVnQ4Vta3p0Q9AShKJSwQjO9-BQdljrtbed8d96__TY3-x6HK_dWPQ6VBb7CmvrsYq6dlZT0H-W9day_lOoJdNby3rFfgHolm2s</recordid><startdate>19830915</startdate><enddate>19830915</enddate><creator>Streeter, David G.</creator><creator>Robins, Roland K.</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>19830915</creationdate><title>Comparative in vitro studies of tiazofurin and a selenazole analog</title><author>Streeter, David G. ; Robins, Roland K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-e177t-ca93044268960031b384b55e057ccf1d32b0f863454efbb8328e492a3a53a78a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1983</creationdate><topic>Animals</topic><topic>Antineoplastic Agents</topic><topic>Cell Survival - drug effects</topic><topic>IMP Dehydrogenase - metabolism</topic><topic>Leukemia L1210 - drug therapy</topic><topic>Leukemia L1210 - enzymology</topic><topic>Leukemia P388 - drug therapy</topic><topic>Leukemia P388 - enzymology</topic><topic>Leukemia, Experimental - drug therapy</topic><topic>Mice</topic><topic>Nucleoside-Diphosphate Kinase - antagonists & inhibitors</topic><topic>Organoselenium Compounds</topic><topic>Ribavirin - analogs & derivatives</topic><topic>Ribavirin - therapeutic use</topic><topic>Ribonucleosides - therapeutic use</topic><topic>Selenium - therapeutic use</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Streeter, David G.</creatorcontrib><creatorcontrib>Robins, Roland K.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Biochemical and biophysical research communications</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Streeter, David G.</au><au>Robins, Roland K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Comparative in vitro studies of tiazofurin and a selenazole analog</atitle><jtitle>Biochemical and biophysical research communications</jtitle><addtitle>Biochem Biophys Res Commun</addtitle><date>1983-09-15</date><risdate>1983</risdate><volume>115</volume><issue>2</issue><spage>544</spage><epage>550</epage><pages>544-550</pages><issn>0006-291X</issn><eissn>1090-2104</eissn><abstract>2-β-D-Ribofuranosylselenazole-4-carboxamide, a selenazole analog of the antitumor agent Tiazofurin, is severalfold more cytotoxic to murine tumor cells in culture than Tiazofurin. 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| ispartof | Biochemical and biophysical research communications, 1983-09, Vol.115 (2), p.544-550 |
| issn | 0006-291X 1090-2104 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Antineoplastic Agents Cell Survival - drug effects IMP Dehydrogenase - metabolism Leukemia L1210 - drug therapy Leukemia L1210 - enzymology Leukemia P388 - drug therapy Leukemia P388 - enzymology Leukemia, Experimental - drug therapy Mice Nucleoside-Diphosphate Kinase - antagonists & inhibitors Organoselenium Compounds Ribavirin - analogs & derivatives Ribavirin - therapeutic use Ribonucleosides - therapeutic use Selenium - therapeutic use |
| title | Comparative in vitro studies of tiazofurin and a selenazole analog |
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