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Design and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies
Objective: The quinoxaline compound with molecular formula C 8 H 6 N 2 O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial. Methods: As a part of our efforts to design new anticancer agents, in this study, we deve...
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| Published in: | Russian journal of bioorganic chemistry 2024, Vol.50 (6), p.2171-2181 |
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| Main Authors: | , , , , , |
| Format: | Article |
| Language: | English |
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| container_end_page | 2181 |
| container_issue | 6 |
| container_start_page | 2171 |
| container_title | Russian journal of bioorganic chemistry |
| container_volume | 50 |
| creator | Dasari, Gouthami Pandiri, Madhuri Badithapuram, Vinitha Karnekanti, Rajender Reddy Mandala, Jyothi Bandari, Srinivas |
| description | Objective:
The quinoxaline compound with molecular formula C
8
H
6
N
2
O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial.
Methods:
As a part of our efforts to design new anticancer agents, in this study, we develop quinoxaline-thiazole-benzamide hybrids. The anticancer evolution of these hybrids was studied using the MTT assay method.
Results and Discussion:
The anticancer activity results exhibit that three compounds, 3,5-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide, 4-methoxy-
N-
(4-(2-oxo-1,2-dihydroquinoxa line-1-carbonyl)thiazol-2-yl)benzamide, and 3,4-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide were shown remarkable anticancer activity ranging from 1.23 to 1.96 µM, demonstrating greater potency than the standard drug.
Conclusions:
Finally, the
in silico
results are strongly supported by
in vitro
anticancer activity data and tyrosine kinase EGFR inhibitory activity assay results. |
| doi_str_mv | 10.1134/S1068162024060104 |
| format | article |
| fullrecord | <record><control><sourceid>proquest_sprin</sourceid><recordid>TN_cdi_proquest_journals_3145726783</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>3145726783</sourcerecordid><originalsourceid>FETCH-LOGICAL-p714-73a42cb4c2002977cc8acc840a560df7fc346dc263a1144e780f9a9950eb786b3</originalsourceid><addsrcrecordid>eNplkM9OwzAMxisEEmPwANwicS44TZq03Mb4s0kDhFohblWaplvGlo6kBbY34K3JGBIHDpZtfT9_thwEpxjOMSb0IsPAEswiiCgwwED3gh5mkISEwMu-r70cbvXD4Mi5OXgE4qQXfF0rp6cGCVOhbG3amW8damqUNUuFHtQHeuq0aT7FQhsV5jMtNs1ChVfKbMRSVwqN1qXVlbtEY4OedWsbNDCtlsJIZdFAtvpdt-sf-3ymtEX3flx2C2HRdSNftZmirO0qrdxxcFCLhVMnv7kf5Lc3-XAUTh7vxsPBJFxxTENOBI1kSWUEEKWcS5kIHxREzKCqeS0JZZWMGBEYU6p4AnUq0jQGVfKElaQfnO1sV7Z565Rri3nTWeM3FgTTmEeMJ8RT0Y5yK-tvVPaPwlBsP178-zj5BvTCdDM</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>3145726783</pqid></control><display><type>article</type><title>Design and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies</title><source>Springer Nature</source><creator>Dasari, Gouthami ; Pandiri, Madhuri ; Badithapuram, Vinitha ; Karnekanti, Rajender Reddy ; Mandala, Jyothi ; Bandari, Srinivas</creator><creatorcontrib>Dasari, Gouthami ; Pandiri, Madhuri ; Badithapuram, Vinitha ; Karnekanti, Rajender Reddy ; Mandala, Jyothi ; Bandari, Srinivas</creatorcontrib><description>Objective:
The quinoxaline compound with molecular formula C
8
H
6
N
2
O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial.
Methods:
As a part of our efforts to design new anticancer agents, in this study, we develop quinoxaline-thiazole-benzamide hybrids. The anticancer evolution of these hybrids was studied using the MTT assay method.
Results and Discussion:
The anticancer activity results exhibit that three compounds, 3,5-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide, 4-methoxy-
N-
(4-(2-oxo-1,2-dihydroquinoxa line-1-carbonyl)thiazol-2-yl)benzamide, and 3,4-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide were shown remarkable anticancer activity ranging from 1.23 to 1.96 µM, demonstrating greater potency than the standard drug.
Conclusions:
Finally, the
in silico
results are strongly supported by
in vitro
anticancer activity data and tyrosine kinase EGFR inhibitory activity assay results.</description><identifier>ISSN: 1068-1620</identifier><identifier>EISSN: 1608-330X</identifier><identifier>DOI: 10.1134/S1068162024060104</identifier><language>eng</language><publisher>Moscow: Pleiades Publishing</publisher><subject>Anticancer properties ; Benzamide ; Biochemistry ; Biomedical and Life Sciences ; Biomedicine ; Bioorganic Chemistry ; Carbonyls ; Chemical synthesis ; Kinases ; Life Sciences ; Molecular docking ; Organic Chemistry ; Quinoxalines ; Tyrosine</subject><ispartof>Russian journal of bioorganic chemistry, 2024, Vol.50 (6), p.2171-2181</ispartof><rights>Pleiades Publishing, Ltd. 2024</rights><rights>Copyright Springer Nature B.V. 2024</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></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></links><search><creatorcontrib>Dasari, Gouthami</creatorcontrib><creatorcontrib>Pandiri, Madhuri</creatorcontrib><creatorcontrib>Badithapuram, Vinitha</creatorcontrib><creatorcontrib>Karnekanti, Rajender Reddy</creatorcontrib><creatorcontrib>Mandala, Jyothi</creatorcontrib><creatorcontrib>Bandari, Srinivas</creatorcontrib><title>Design and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies</title><title>Russian journal of bioorganic chemistry</title><addtitle>Russ J Bioorg Chem</addtitle><description>Objective:
The quinoxaline compound with molecular formula C
8
H
6
N
2
O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial.
Methods:
As a part of our efforts to design new anticancer agents, in this study, we develop quinoxaline-thiazole-benzamide hybrids. The anticancer evolution of these hybrids was studied using the MTT assay method.
Results and Discussion:
The anticancer activity results exhibit that three compounds, 3,5-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide, 4-methoxy-
N-
(4-(2-oxo-1,2-dihydroquinoxa line-1-carbonyl)thiazol-2-yl)benzamide, and 3,4-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide were shown remarkable anticancer activity ranging from 1.23 to 1.96 µM, demonstrating greater potency than the standard drug.
Conclusions:
Finally, the
in silico
results are strongly supported by
in vitro
anticancer activity data and tyrosine kinase EGFR inhibitory activity assay results.</description><subject>Anticancer properties</subject><subject>Benzamide</subject><subject>Biochemistry</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Bioorganic Chemistry</subject><subject>Carbonyls</subject><subject>Chemical synthesis</subject><subject>Kinases</subject><subject>Life Sciences</subject><subject>Molecular docking</subject><subject>Organic Chemistry</subject><subject>Quinoxalines</subject><subject>Tyrosine</subject><issn>1068-1620</issn><issn>1608-330X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid/><recordid>eNplkM9OwzAMxisEEmPwANwicS44TZq03Mb4s0kDhFohblWaplvGlo6kBbY34K3JGBIHDpZtfT9_thwEpxjOMSb0IsPAEswiiCgwwED3gh5mkISEwMu-r70cbvXD4Mi5OXgE4qQXfF0rp6cGCVOhbG3amW8damqUNUuFHtQHeuq0aT7FQhsV5jMtNs1ChVfKbMRSVwqN1qXVlbtEY4OedWsbNDCtlsJIZdFAtvpdt-sf-3ymtEX3flx2C2HRdSNftZmirO0qrdxxcFCLhVMnv7kf5Lc3-XAUTh7vxsPBJFxxTENOBI1kSWUEEKWcS5kIHxREzKCqeS0JZZWMGBEYU6p4AnUq0jQGVfKElaQfnO1sV7Z565Rri3nTWeM3FgTTmEeMJ8RT0Y5yK-tvVPaPwlBsP178-zj5BvTCdDM</recordid><startdate>2024</startdate><enddate>2024</enddate><creator>Dasari, Gouthami</creator><creator>Pandiri, Madhuri</creator><creator>Badithapuram, Vinitha</creator><creator>Karnekanti, Rajender Reddy</creator><creator>Mandala, Jyothi</creator><creator>Bandari, Srinivas</creator><general>Pleiades Publishing</general><general>Springer Nature B.V</general><scope/></search><sort><creationdate>2024</creationdate><title>Design and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies</title><author>Dasari, Gouthami ; Pandiri, Madhuri ; Badithapuram, Vinitha ; Karnekanti, Rajender Reddy ; Mandala, Jyothi ; Bandari, Srinivas</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p714-73a42cb4c2002977cc8acc840a560df7fc346dc263a1144e780f9a9950eb786b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Anticancer properties</topic><topic>Benzamide</topic><topic>Biochemistry</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Bioorganic Chemistry</topic><topic>Carbonyls</topic><topic>Chemical synthesis</topic><topic>Kinases</topic><topic>Life Sciences</topic><topic>Molecular docking</topic><topic>Organic Chemistry</topic><topic>Quinoxalines</topic><topic>Tyrosine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Dasari, Gouthami</creatorcontrib><creatorcontrib>Pandiri, Madhuri</creatorcontrib><creatorcontrib>Badithapuram, Vinitha</creatorcontrib><creatorcontrib>Karnekanti, Rajender Reddy</creatorcontrib><creatorcontrib>Mandala, Jyothi</creatorcontrib><creatorcontrib>Bandari, Srinivas</creatorcontrib><jtitle>Russian journal of bioorganic chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Dasari, Gouthami</au><au>Pandiri, Madhuri</au><au>Badithapuram, Vinitha</au><au>Karnekanti, Rajender Reddy</au><au>Mandala, Jyothi</au><au>Bandari, Srinivas</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Design and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies</atitle><jtitle>Russian journal of bioorganic chemistry</jtitle><stitle>Russ J Bioorg Chem</stitle><date>2024</date><risdate>2024</risdate><volume>50</volume><issue>6</issue><spage>2171</spage><epage>2181</epage><pages>2171-2181</pages><issn>1068-1620</issn><eissn>1608-330X</eissn><abstract>Objective:
The quinoxaline compound with molecular formula C
8
H
6
N
2
O, which shows a wide range of biological activities including antiviral, anticancer, antimicrobial, antituberculosis, and antileishmanial.
Methods:
As a part of our efforts to design new anticancer agents, in this study, we develop quinoxaline-thiazole-benzamide hybrids. The anticancer evolution of these hybrids was studied using the MTT assay method.
Results and Discussion:
The anticancer activity results exhibit that three compounds, 3,5-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide, 4-methoxy-
N-
(4-(2-oxo-1,2-dihydroquinoxa line-1-carbonyl)thiazol-2-yl)benzamide, and 3,4-dimethoxy-
N
-(4-(2-oxo-1,2-dihydroquinoxaline-1-carbonyl)thiazol-2-yl)benzamide were shown remarkable anticancer activity ranging from 1.23 to 1.96 µM, demonstrating greater potency than the standard drug.
Conclusions:
Finally, the
in silico
results are strongly supported by
in vitro
anticancer activity data and tyrosine kinase EGFR inhibitory activity assay results.</abstract><cop>Moscow</cop><pub>Pleiades Publishing</pub><doi>10.1134/S1068162024060104</doi><tpages>11</tpages></addata></record> |
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| issn | 1068-1620 1608-330X |
| language | eng |
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| source | Springer Nature |
| subjects | Anticancer properties Benzamide Biochemistry Biomedical and Life Sciences Biomedicine Bioorganic Chemistry Carbonyls Chemical synthesis Kinases Life Sciences Molecular docking Organic Chemistry Quinoxalines Tyrosine |
| title | Design and Synthesis of Some New Quinoxaline-Thiazole-Benzamide Hybrids: In Vitro Anticancer Activity and Their Molecular Docking Studies |
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