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Gallic acid-based indanone derivatives as anticancer agents
Gallic acid-based indanone derivatives have been synthesised. Indanones 10, 11, 12 and 14 showed potent anticancer activity (IC 50 = 0.022–2.2 μM) against human cancer cell lines. The most active indanone against MCF-7, that is, hormone-dependent breast cancer cell line ( 10, IC 50 = 2.2 μM) showed...
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Published in: | Bioorganic & medicinal chemistry 2008-07, Vol.18 (14), p.3914-3918 |
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container_start_page | 3914 |
container_title | Bioorganic & medicinal chemistry |
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creator | Saxena, Hari Om Faridi, Uzma Srivastava, Suchita Kumar, J.K. Darokar, M.P. Luqman, Suaib Chanotiya, C.S. Krishna, Vinay Negi, Arvind S. Khanuja, S.P.S. |
description | Gallic acid-based indanone derivatives have been synthesised. Indanones
10,
11,
12 and
14 showed potent anticancer activity (IC
50
=
0.022–2.2
μM) against human cancer cell lines. The most active indanone against MCF-7, that is, hormone-dependent breast cancer cell line (
10, IC
50
=
2.2
μM) showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, some of the indanones exhibited toxicity to erythrocytes at higher concentrations. Gallic acid-based indanones may further be optimised as better anticancer agents with low toxicity.
Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds
10,
11,
12 and
14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone (
10, IC
50
=
2.2
μM), against MCF-7, that is, hormone-dependent breast cancer cell line, showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, indanones
11,
12 and
14 showed toxicities to erythrocytes at higher concentrations. |
doi_str_mv | 10.1016/j.bmcl.2008.06.039 |
format | article |
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10,
11,
12 and
14 showed potent anticancer activity (IC
50
=
0.022–2.2
μM) against human cancer cell lines. The most active indanone against MCF-7, that is, hormone-dependent breast cancer cell line (
10, IC
50
=
2.2
μM) showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, some of the indanones exhibited toxicity to erythrocytes at higher concentrations. Gallic acid-based indanones may further be optimised as better anticancer agents with low toxicity.
Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds
10,
11,
12 and
14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone (
10, IC
50
=
2.2
μM), against MCF-7, that is, hormone-dependent breast cancer cell line, showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, indanones
11,
12 and
14 showed toxicities to erythrocytes at higher concentrations.</description><identifier>ISSN: 0960-894X</identifier><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3405</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmcl.2008.06.039</identifier><identifier>PMID: 18586491</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Anticancer ; Antineoplastic agents ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - pharmacology ; Antioxidants - pharmacology ; Biological and medical sciences ; Cell Line, Tumor ; Chemistry, Pharmaceutical - methods ; Drug Design ; Drug Screening Assays, Antitumor ; Erythrocytes - drug effects ; Gallic acid ; Gallic Acid - chemistry ; General aspects ; Hemolysis ; HMQC ; Humans ; Indanones ; Indans - chemical synthesis ; Indans - chemistry ; Inhibitory Concentration 50 ; Medical sciences ; Models, Chemical ; Osmosis ; Osmotic fragility ; Pharmacology. Drug treatments ; Tetrazolium Salts - pharmacology ; Thiazoles - pharmacology</subject><ispartof>Bioorganic & medicinal chemistry, 2008-07, Vol.18 (14), p.3914-3918</ispartof><rights>2008 Elsevier Ltd</rights><rights>2008 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c481t-c6fa4417e628d83e94e8763388835a0d3ca17b8dba0d138c24dcd3fab30026ad3</citedby><cites>FETCH-LOGICAL-c481t-c6fa4417e628d83e94e8763388835a0d3ca17b8dba0d138c24dcd3fab30026ad3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=20544058$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18586491$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Saxena, Hari Om</creatorcontrib><creatorcontrib>Faridi, Uzma</creatorcontrib><creatorcontrib>Srivastava, Suchita</creatorcontrib><creatorcontrib>Kumar, J.K.</creatorcontrib><creatorcontrib>Darokar, M.P.</creatorcontrib><creatorcontrib>Luqman, Suaib</creatorcontrib><creatorcontrib>Chanotiya, C.S.</creatorcontrib><creatorcontrib>Krishna, Vinay</creatorcontrib><creatorcontrib>Negi, Arvind S.</creatorcontrib><creatorcontrib>Khanuja, S.P.S.</creatorcontrib><title>Gallic acid-based indanone derivatives as anticancer agents</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Gallic acid-based indanone derivatives have been synthesised. Indanones
10,
11,
12 and
14 showed potent anticancer activity (IC
50
=
0.022–2.2
μM) against human cancer cell lines. The most active indanone against MCF-7, that is, hormone-dependent breast cancer cell line (
10, IC
50
=
2.2
μM) showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, some of the indanones exhibited toxicity to erythrocytes at higher concentrations. Gallic acid-based indanones may further be optimised as better anticancer agents with low toxicity.
Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds
10,
11,
12 and
14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone (
10, IC
50
=
2.2
μM), against MCF-7, that is, hormone-dependent breast cancer cell line, showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, indanones
11,
12 and
14 showed toxicities to erythrocytes at higher concentrations.</description><subject>Anticancer</subject><subject>Antineoplastic agents</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Antioxidants - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cell Line, Tumor</subject><subject>Chemistry, Pharmaceutical - methods</subject><subject>Drug Design</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Erythrocytes - drug effects</subject><subject>Gallic acid</subject><subject>Gallic Acid - chemistry</subject><subject>General aspects</subject><subject>Hemolysis</subject><subject>HMQC</subject><subject>Humans</subject><subject>Indanones</subject><subject>Indans - chemical synthesis</subject><subject>Indans - chemistry</subject><subject>Inhibitory Concentration 50</subject><subject>Medical sciences</subject><subject>Models, Chemical</subject><subject>Osmosis</subject><subject>Osmotic fragility</subject><subject>Pharmacology. Drug treatments</subject><subject>Tetrazolium Salts - pharmacology</subject><subject>Thiazoles - pharmacology</subject><issn>0960-894X</issn><issn>0968-0896</issn><issn>1464-3405</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><recordid>eNp9kE1LxDAQhoMoun78AQ_Si95aJ02aTdGLiK6C4EXBW5gmU8nSbdeku-C_N8suehMGZg7POzM8jJ1zKDhwdT0vmoXtihJAF6AKEPUem3CpZC4kVPtsArWCXNfy44gdxzgH4BKkPGRHXFdayZpP2M0Mu87bDK13eYORXOZ7h_3QU-Yo-DWOfk0xw1T96C32lkKGn9SP8ZQdtNhFOtv1E_b--PB2_5S_vM6e7-9ecis1H3OrWpSST0mV2mlBtSQ9VUJorUWF4IRFPm20a9LMhbaldNaJFhsBUCp04oRdbfcuw_C1ojiahY-Wug57GlbR8FoIqGSdwHIL2jDEGKg1y-AXGL4NB7NRZuZmo8xslBlQJilLoYvd9lWzIPcX2TlKwOUOwGixa0Ny4OMvV6bTSbdO3O2Wo-Ri7SmYaD0lX84HsqNxg__vjx_eLYle</recordid><startdate>20080715</startdate><enddate>20080715</enddate><creator>Saxena, Hari Om</creator><creator>Faridi, Uzma</creator><creator>Srivastava, Suchita</creator><creator>Kumar, J.K.</creator><creator>Darokar, M.P.</creator><creator>Luqman, Suaib</creator><creator>Chanotiya, C.S.</creator><creator>Krishna, Vinay</creator><creator>Negi, Arvind S.</creator><creator>Khanuja, S.P.S.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20080715</creationdate><title>Gallic acid-based indanone derivatives as anticancer agents</title><author>Saxena, Hari Om ; Faridi, Uzma ; Srivastava, Suchita ; Kumar, J.K. ; Darokar, M.P. ; Luqman, Suaib ; Chanotiya, C.S. ; Krishna, Vinay ; Negi, Arvind S. ; Khanuja, S.P.S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c481t-c6fa4417e628d83e94e8763388835a0d3ca17b8dba0d138c24dcd3fab30026ad3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2008</creationdate><topic>Anticancer</topic><topic>Antineoplastic agents</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Antioxidants - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cell Line, Tumor</topic><topic>Chemistry, Pharmaceutical - methods</topic><topic>Drug Design</topic><topic>Drug Screening Assays, Antitumor</topic><topic>Erythrocytes - drug effects</topic><topic>Gallic acid</topic><topic>Gallic Acid - chemistry</topic><topic>General aspects</topic><topic>Hemolysis</topic><topic>HMQC</topic><topic>Humans</topic><topic>Indanones</topic><topic>Indans - chemical synthesis</topic><topic>Indans - chemistry</topic><topic>Inhibitory Concentration 50</topic><topic>Medical sciences</topic><topic>Models, Chemical</topic><topic>Osmosis</topic><topic>Osmotic fragility</topic><topic>Pharmacology. Drug treatments</topic><topic>Tetrazolium Salts - pharmacology</topic><topic>Thiazoles - pharmacology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Saxena, Hari Om</creatorcontrib><creatorcontrib>Faridi, Uzma</creatorcontrib><creatorcontrib>Srivastava, Suchita</creatorcontrib><creatorcontrib>Kumar, J.K.</creatorcontrib><creatorcontrib>Darokar, M.P.</creatorcontrib><creatorcontrib>Luqman, Suaib</creatorcontrib><creatorcontrib>Chanotiya, C.S.</creatorcontrib><creatorcontrib>Krishna, Vinay</creatorcontrib><creatorcontrib>Negi, Arvind S.</creatorcontrib><creatorcontrib>Khanuja, S.P.S.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Saxena, Hari Om</au><au>Faridi, Uzma</au><au>Srivastava, Suchita</au><au>Kumar, J.K.</au><au>Darokar, M.P.</au><au>Luqman, Suaib</au><au>Chanotiya, C.S.</au><au>Krishna, Vinay</au><au>Negi, Arvind S.</au><au>Khanuja, S.P.S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Gallic acid-based indanone derivatives as anticancer agents</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2008-07-15</date><risdate>2008</risdate><volume>18</volume><issue>14</issue><spage>3914</spage><epage>3918</epage><pages>3914-3918</pages><issn>0960-894X</issn><issn>0968-0896</issn><eissn>1464-3405</eissn><eissn>1464-3391</eissn><abstract>Gallic acid-based indanone derivatives have been synthesised. Indanones
10,
11,
12 and
14 showed potent anticancer activity (IC
50
=
0.022–2.2
μM) against human cancer cell lines. The most active indanone against MCF-7, that is, hormone-dependent breast cancer cell line (
10, IC
50
=
2.2
μM) showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, some of the indanones exhibited toxicity to erythrocytes at higher concentrations. Gallic acid-based indanones may further be optimised as better anticancer agents with low toxicity.
Gallic acid-based indanone derivatives have been synthesised. Some of the indanones showed very good anticancer activity in MTT assay. Compounds
10,
11,
12 and
14 possessed potent anticancer activity against various human cancer cell lines. The most potent indanone (
10, IC
50
=
2.2
μM), against MCF-7, that is, hormone-dependent breast cancer cell line, showed no toxicity to human erythrocytes even at higher concentrations (100
μg/ml, 258
μM). While, indanones
11,
12 and
14 showed toxicities to erythrocytes at higher concentrations.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>18586491</pmid><doi>10.1016/j.bmcl.2008.06.039</doi><tpages>5</tpages></addata></record> |
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identifier | ISSN: 0960-894X |
ispartof | Bioorganic & medicinal chemistry, 2008-07, Vol.18 (14), p.3914-3918 |
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language | eng |
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source | ScienceDirect Journals |
subjects | Anticancer Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Antioxidants - pharmacology Biological and medical sciences Cell Line, Tumor Chemistry, Pharmaceutical - methods Drug Design Drug Screening Assays, Antitumor Erythrocytes - drug effects Gallic acid Gallic Acid - chemistry General aspects Hemolysis HMQC Humans Indanones Indans - chemical synthesis Indans - chemistry Inhibitory Concentration 50 Medical sciences Models, Chemical Osmosis Osmotic fragility Pharmacology. Drug treatments Tetrazolium Salts - pharmacology Thiazoles - pharmacology |
title | Gallic acid-based indanone derivatives as anticancer agents |
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