Synthesis and biological evaluation of indolyl chalcones as antitumor agents
A series of indolyl chalcones were synthesized and evaluated for their in vitro anti-proliferative activities against various cancer cell lines. A series of indolyl chalcones were synthesized and evaluated in vitro for their anticancer activity against three human cancer cell lines. Compounds 3b– d,...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (13), p.3916-3919 |
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container_title | Bioorganic & medicinal chemistry letters |
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creator | Kumar, Dalip Kumar, N. Maruthi Akamatsu, Kanako Kusaka, Eriko Harada, Hiroshi Ito, Takeo |
description | A series of indolyl chalcones were synthesized and evaluated for their in vitro anti-proliferative activities against various cancer cell lines.
A series of indolyl chalcones were synthesized and evaluated in vitro for their anticancer activity against three human cancer cell lines. Compounds
3b–
d,
3h,
3j,
3l,
3m,
4g, and
4j showed significant cytotoxicity, particularly, indolyl chalcones
3l and
3m were identified as the most potent and selective anticancer agents with IC
50 values 0.03 and 0.09
μM, against PaCa-2 cell line, respectively. |
doi_str_mv | 10.1016/j.bmcl.2010.05.016 |
format | Article |
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A series of indolyl chalcones were synthesized and evaluated in vitro for their anticancer activity against three human cancer cell lines. Compounds
3b–
d,
3h,
3j,
3l,
3m,
4g, and
4j showed significant cytotoxicity, particularly, indolyl chalcones
3l and
3m were identified as the most potent and selective anticancer agents with IC
50 values 0.03 and 0.09
μM, against PaCa-2 cell line, respectively.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.05.016</identifier><identifier>PMID: 20627724</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>1,3-Diaryl-2-propen-1-ones ; Anticancer agents ; Antineoplastic agents ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Biological and medical sciences ; Cell Line, Tumor ; Cell Proliferation - drug effects ; Chalcones - chemical synthesis ; Chalcones - chemistry ; Chalcones - pharmacology ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; General aspects ; Humans ; Indolyl chalcones ; Medical sciences ; Molecular Structure ; Pharmacology. Drug treatments ; Stereoisomerism ; Structure-Activity Relationship</subject><ispartof>Bioorganic & medicinal chemistry letters, 2010-07, Vol.20 (13), p.3916-3919</ispartof><rights>2010 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>2010 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c527t-870b149590036930f3ad9e1c4a477786c7a590ace2759151cadef3659998a4583</citedby><cites>FETCH-LOGICAL-c527t-870b149590036930f3ad9e1c4a477786c7a590ace2759151cadef3659998a4583</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X10006578$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22990229$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/20627724$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kumar, Dalip</creatorcontrib><creatorcontrib>Kumar, N. Maruthi</creatorcontrib><creatorcontrib>Akamatsu, Kanako</creatorcontrib><creatorcontrib>Kusaka, Eriko</creatorcontrib><creatorcontrib>Harada, Hiroshi</creatorcontrib><creatorcontrib>Ito, Takeo</creatorcontrib><title>Synthesis and biological evaluation of indolyl chalcones as antitumor agents</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A series of indolyl chalcones were synthesized and evaluated for their in vitro anti-proliferative activities against various cancer cell lines.
A series of indolyl chalcones were synthesized and evaluated in vitro for their anticancer activity against three human cancer cell lines. Compounds
3b–
d,
3h,
3j,
3l,
3m,
4g, and
4j showed significant cytotoxicity, particularly, indolyl chalcones
3l and
3m were identified as the most potent and selective anticancer agents with IC
50 values 0.03 and 0.09
μM, against PaCa-2 cell line, respectively.</description><subject>1,3-Diaryl-2-propen-1-ones</subject><subject>Anticancer agents</subject><subject>Antineoplastic agents</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Chalcones - chemical synthesis</subject><subject>Chalcones - chemistry</subject><subject>Chalcones - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Screening Assays, Antitumor</subject><subject>General aspects</subject><subject>Humans</subject><subject>Indolyl chalcones</subject><subject>Medical sciences</subject><subject>Molecular Structure</subject><subject>Pharmacology. Drug treatments</subject><subject>Stereoisomerism</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEFrFDEYhoModq3-AQ8yF-lp1i8zyWQCXqS0Vljw0ArewreZb9osmaQmM4X992bZVW_1ksCb530JD2PvOaw58O7Tbr2drF83UAKQ6xK9YCsuOlG3AuRLtgLdQd1r8fOMvcl5B8AFCPGanTXQNUo1YsU2t_swP1B2ucIwVFsXfbx3Fn1FT-gXnF0MVRwrF4bo976yD-htDFTwQ2N28zLFVOE9hTm_Za9G9Jnene5z9uP66u7ypt58__rt8sumtrJRc90r2HKhpQZoO93C2OKgiVuBQinVd1ZheUNLjZKaS25xoLHtpNa6RyH79pxdHHcfU_y1UJ7N5LIl7zFQXLJRUvRluJX_J0WvO6WlKmRzJG2KOScazWNyE6a94WAOus3OHHSbg24D0pSolD6c5pftRMPfyh-_Bfh4AjAXqWPCYF3-xzVaQzkK9_nIUdH25CiZbB0FS4NLZGczRPfcP34DBImc6w</recordid><startdate>20100701</startdate><enddate>20100701</enddate><creator>Kumar, Dalip</creator><creator>Kumar, N. 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Maruthi ; Akamatsu, Kanako ; Kusaka, Eriko ; Harada, Hiroshi ; Ito, Takeo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c527t-870b149590036930f3ad9e1c4a477786c7a590ace2759151cadef3659998a4583</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>1,3-Diaryl-2-propen-1-ones</topic><topic>Anticancer agents</topic><topic>Antineoplastic agents</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - chemistry</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cell Line, Tumor</topic><topic>Cell Proliferation - drug effects</topic><topic>Chalcones - chemical synthesis</topic><topic>Chalcones - chemistry</topic><topic>Chalcones - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>Drug Screening Assays, Antitumor</topic><topic>General aspects</topic><topic>Humans</topic><topic>Indolyl chalcones</topic><topic>Medical sciences</topic><topic>Molecular Structure</topic><topic>Pharmacology. Drug treatments</topic><topic>Stereoisomerism</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kumar, Dalip</creatorcontrib><creatorcontrib>Kumar, N. Maruthi</creatorcontrib><creatorcontrib>Akamatsu, Kanako</creatorcontrib><creatorcontrib>Kusaka, Eriko</creatorcontrib><creatorcontrib>Harada, Hiroshi</creatorcontrib><creatorcontrib>Ito, Takeo</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>MEDLINE - Academic</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 letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kumar, Dalip</au><au>Kumar, N. 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A series of indolyl chalcones were synthesized and evaluated in vitro for their anticancer activity against three human cancer cell lines. Compounds
3b–
d,
3h,
3j,
3l,
3m,
4g, and
4j showed significant cytotoxicity, particularly, indolyl chalcones
3l and
3m were identified as the most potent and selective anticancer agents with IC
50 values 0.03 and 0.09
μM, against PaCa-2 cell line, respectively.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>20627724</pmid><doi>10.1016/j.bmcl.2010.05.016</doi><tpages>4</tpages></addata></record> |
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subjects | 1,3-Diaryl-2-propen-1-ones Anticancer agents Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Cell Line, Tumor Cell Proliferation - drug effects Chalcones - chemical synthesis Chalcones - chemistry Chalcones - pharmacology Dose-Response Relationship, Drug Drug Screening Assays, Antitumor General aspects Humans Indolyl chalcones Medical sciences Molecular Structure Pharmacology. Drug treatments Stereoisomerism Structure-Activity Relationship |
title | Synthesis and biological evaluation of indolyl chalcones as antitumor agents |
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