Studies on imidazo[2,1-b][1,3]benzothiazole derivatives as new radiosensitizers
The synthesis and characterization of potent 7-substituted-2-(4-substitutedphenyl)imidazo[2,1- b ][1,3]benzothiazoles as effective radiosensitizers and anticarcinogenic compound is reported. The activity is determined against human liver cancer Hep G2 cell line, two parental melanoma cell lines (hum...
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| Veröffentlicht in: | SN applied sciences 2020-11, Vol.2 (11), p.1902, Article 1902 |
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| creator | Majalakere, Krishnakishore Kunhana, Sarojini Balladka Rao, Shama Kalal, Bhuvanesh Sukhlal Badiadka, Narayana Sanjeev, Ganesh Holla, Bantwal Shivaram |
| description | The synthesis and characterization of potent 7-substituted-2-(4-substitutedphenyl)imidazo[2,1-
b
][1,3]benzothiazoles as effective radiosensitizers and anticarcinogenic compound is reported. The activity is determined against human liver cancer Hep G2 cell line, two parental melanoma cell lines (human melanoma cell line, A375C and mouse melanoma cell line, A375C). The compounds 7-sulfonamide-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3f
, IC
50
= 0.097 μM) and 7-sulfonamide-2-(4-methylphenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3g
, IC
50
= 0.114 μM) exhibited considerable
in vitro
anticancer activity against Hep G2 cell line while 7-bromo-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole showed effectiveness against both parental melanoma cell lines (
3c
, IC
50
= 0.04 and 0.052 μM). Further the active molecules
3f, 3g
and
3h
are tested for radiosensitizing activity over Hep G2 cell line at 4 Gy, with the comet formed at 0.054 μM . Similarly,
3c
tested against two parental melanoma cell lines, it has proven to be more potent when combined with 2 Gy ϒ-radiation. The present study reveals that presence of sulfonamide in combination with methoxy substitution enhanced DNA fragmentation and there by acting as effective derivative for Hepatocellular carcinoma. |
| doi_str_mv | 10.1007/s42452-020-03726-7 |
| format | Article |
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b
][1,3]benzothiazoles as effective radiosensitizers and anticarcinogenic compound is reported. The activity is determined against human liver cancer Hep G2 cell line, two parental melanoma cell lines (human melanoma cell line, A375C and mouse melanoma cell line, A375C). The compounds 7-sulfonamide-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3f
, IC
50
= 0.097 μM) and 7-sulfonamide-2-(4-methylphenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3g
, IC
50
= 0.114 μM) exhibited considerable
in vitro
anticancer activity against Hep G2 cell line while 7-bromo-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole showed effectiveness against both parental melanoma cell lines (
3c
, IC
50
= 0.04 and 0.052 μM). Further the active molecules
3f, 3g
and
3h
are tested for radiosensitizing activity over Hep G2 cell line at 4 Gy, with the comet formed at 0.054 μM . Similarly,
3c
tested against two parental melanoma cell lines, it has proven to be more potent when combined with 2 Gy ϒ-radiation. The present study reveals that presence of sulfonamide in combination with methoxy substitution enhanced DNA fragmentation and there by acting as effective derivative for Hepatocellular carcinoma.</description><identifier>ISSN: 2523-3963</identifier><identifier>EISSN: 2523-3971</identifier><identifier>DOI: 10.1007/s42452-020-03726-7</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Anticancer properties ; Antitumor activity ; Apoptosis ; Applied and Technical Physics ; Benzothiazole ; Cancer therapies ; Carbon ; Chemistry/Food Science ; Chemistry: Pharmaceutical ; DNA fragmentation ; Drug dosages ; Earth Sciences ; Engineering ; Environment ; Hepatocellular carcinoma ; Hepatocytes ; Hypoxia ; Liver cancer ; Materials Science ; Medical ; Medicinal and Clinical Chemistry ; Melanoma ; Radiation ; Radiosensitizers ; Research Article ; Sulfonamides</subject><ispartof>SN applied sciences, 2020-11, Vol.2 (11), p.1902, Article 1902</ispartof><rights>Springer Nature Switzerland AG 2020</rights><rights>Springer Nature Switzerland AG 2020.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c363t-f9fbafb89f9cd09bcc484e23886294f79ccf220c876dd64b41d69cc80a8f5393</citedby><cites>FETCH-LOGICAL-c363t-f9fbafb89f9cd09bcc484e23886294f79ccf220c876dd64b41d69cc80a8f5393</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids></links><search><creatorcontrib>Majalakere, Krishnakishore</creatorcontrib><creatorcontrib>Kunhana, Sarojini Balladka</creatorcontrib><creatorcontrib>Rao, Shama</creatorcontrib><creatorcontrib>Kalal, Bhuvanesh Sukhlal</creatorcontrib><creatorcontrib>Badiadka, Narayana</creatorcontrib><creatorcontrib>Sanjeev, Ganesh</creatorcontrib><creatorcontrib>Holla, Bantwal Shivaram</creatorcontrib><title>Studies on imidazo[2,1-b][1,3]benzothiazole derivatives as new radiosensitizers</title><title>SN applied sciences</title><addtitle>SN Appl. Sci</addtitle><description>The synthesis and characterization of potent 7-substituted-2-(4-substitutedphenyl)imidazo[2,1-
b
][1,3]benzothiazoles as effective radiosensitizers and anticarcinogenic compound is reported. The activity is determined against human liver cancer Hep G2 cell line, two parental melanoma cell lines (human melanoma cell line, A375C and mouse melanoma cell line, A375C). The compounds 7-sulfonamide-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3f
, IC
50
= 0.097 μM) and 7-sulfonamide-2-(4-methylphenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3g
, IC
50
= 0.114 μM) exhibited considerable
in vitro
anticancer activity against Hep G2 cell line while 7-bromo-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole showed effectiveness against both parental melanoma cell lines (
3c
, IC
50
= 0.04 and 0.052 μM). Further the active molecules
3f, 3g
and
3h
are tested for radiosensitizing activity over Hep G2 cell line at 4 Gy, with the comet formed at 0.054 μM . Similarly,
3c
tested against two parental melanoma cell lines, it has proven to be more potent when combined with 2 Gy ϒ-radiation. The present study reveals that presence of sulfonamide in combination with methoxy substitution enhanced DNA fragmentation and there by acting as effective derivative for Hepatocellular carcinoma.</description><subject>Anticancer properties</subject><subject>Antitumor activity</subject><subject>Apoptosis</subject><subject>Applied and Technical Physics</subject><subject>Benzothiazole</subject><subject>Cancer therapies</subject><subject>Carbon</subject><subject>Chemistry/Food Science</subject><subject>Chemistry: Pharmaceutical</subject><subject>DNA fragmentation</subject><subject>Drug dosages</subject><subject>Earth Sciences</subject><subject>Engineering</subject><subject>Environment</subject><subject>Hepatocellular carcinoma</subject><subject>Hepatocytes</subject><subject>Hypoxia</subject><subject>Liver cancer</subject><subject>Materials Science</subject><subject>Medical</subject><subject>Medicinal and Clinical Chemistry</subject><subject>Melanoma</subject><subject>Radiation</subject><subject>Radiosensitizers</subject><subject>Research Article</subject><subject>Sulfonamides</subject><issn>2523-3963</issn><issn>2523-3971</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><recordid>eNp9kMtKAzEUhoMoWKov4GrAbaO5NZelFG9Q6MLuSgmZXDSlnanJtGKf3tQR3bk6h8P3_wc-AK4wusEIidvMCBsTiAiCiArCoTgBAzImFFIl8Onvzuk5uMx5hRAiQlEm6QDMXrqdiz5XbVPFTXTm0C7ICMN6ucAjuqx9c2i7t1jOa185n-LedHFfeJOrxn9UybjYZt_k2MWDT_kCnAWzzv7yZw7B_OF-PnmC09nj8-RuCi3ltINBhdqEWqqgrEOqtpZJ5gmVkhPFglDWBkKQlYI7x1nNsOPlJpGRYUwVHYLrvnab2vedz51etbvUlI-aCCkZRUoeKdJTNrU5Jx_0NsWNSZ8aI31Up3t1uqjT3-q0KCHah3KBm1ef_qr_SX0BeYhxlg</recordid><startdate>20201101</startdate><enddate>20201101</enddate><creator>Majalakere, Krishnakishore</creator><creator>Kunhana, Sarojini Balladka</creator><creator>Rao, Shama</creator><creator>Kalal, Bhuvanesh Sukhlal</creator><creator>Badiadka, Narayana</creator><creator>Sanjeev, Ganesh</creator><creator>Holla, Bantwal Shivaram</creator><general>Springer International Publishing</general><general>Springer Nature B.V</general><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20201101</creationdate><title>Studies on imidazo[2,1-b][1,3]benzothiazole derivatives as new radiosensitizers</title><author>Majalakere, Krishnakishore ; Kunhana, Sarojini Balladka ; Rao, Shama ; Kalal, Bhuvanesh Sukhlal ; Badiadka, Narayana ; Sanjeev, Ganesh ; Holla, Bantwal Shivaram</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c363t-f9fbafb89f9cd09bcc484e23886294f79ccf220c876dd64b41d69cc80a8f5393</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Anticancer properties</topic><topic>Antitumor activity</topic><topic>Apoptosis</topic><topic>Applied and Technical Physics</topic><topic>Benzothiazole</topic><topic>Cancer therapies</topic><topic>Carbon</topic><topic>Chemistry/Food Science</topic><topic>Chemistry: Pharmaceutical</topic><topic>DNA fragmentation</topic><topic>Drug dosages</topic><topic>Earth Sciences</topic><topic>Engineering</topic><topic>Environment</topic><topic>Hepatocellular carcinoma</topic><topic>Hepatocytes</topic><topic>Hypoxia</topic><topic>Liver cancer</topic><topic>Materials Science</topic><topic>Medical</topic><topic>Medicinal and Clinical Chemistry</topic><topic>Melanoma</topic><topic>Radiation</topic><topic>Radiosensitizers</topic><topic>Research Article</topic><topic>Sulfonamides</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Majalakere, Krishnakishore</creatorcontrib><creatorcontrib>Kunhana, Sarojini Balladka</creatorcontrib><creatorcontrib>Rao, Shama</creatorcontrib><creatorcontrib>Kalal, Bhuvanesh Sukhlal</creatorcontrib><creatorcontrib>Badiadka, Narayana</creatorcontrib><creatorcontrib>Sanjeev, Ganesh</creatorcontrib><creatorcontrib>Holla, Bantwal Shivaram</creatorcontrib><collection>CrossRef</collection><jtitle>SN applied sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Majalakere, Krishnakishore</au><au>Kunhana, Sarojini Balladka</au><au>Rao, Shama</au><au>Kalal, Bhuvanesh Sukhlal</au><au>Badiadka, Narayana</au><au>Sanjeev, Ganesh</au><au>Holla, Bantwal Shivaram</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Studies on imidazo[2,1-b][1,3]benzothiazole derivatives as new radiosensitizers</atitle><jtitle>SN applied sciences</jtitle><stitle>SN Appl. Sci</stitle><date>2020-11-01</date><risdate>2020</risdate><volume>2</volume><issue>11</issue><spage>1902</spage><pages>1902-</pages><artnum>1902</artnum><issn>2523-3963</issn><eissn>2523-3971</eissn><abstract>The synthesis and characterization of potent 7-substituted-2-(4-substitutedphenyl)imidazo[2,1-
b
][1,3]benzothiazoles as effective radiosensitizers and anticarcinogenic compound is reported. The activity is determined against human liver cancer Hep G2 cell line, two parental melanoma cell lines (human melanoma cell line, A375C and mouse melanoma cell line, A375C). The compounds 7-sulfonamide-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3f
, IC
50
= 0.097 μM) and 7-sulfonamide-2-(4-methylphenyl)imidazo[2,1-
b
][1,3]benzothiazole (
3g
, IC
50
= 0.114 μM) exhibited considerable
in vitro
anticancer activity against Hep G2 cell line while 7-bromo-2-(4-fluorophenyl)imidazo[2,1-
b
][1,3]benzothiazole showed effectiveness against both parental melanoma cell lines (
3c
, IC
50
= 0.04 and 0.052 μM). Further the active molecules
3f, 3g
and
3h
are tested for radiosensitizing activity over Hep G2 cell line at 4 Gy, with the comet formed at 0.054 μM . Similarly,
3c
tested against two parental melanoma cell lines, it has proven to be more potent when combined with 2 Gy ϒ-radiation. The present study reveals that presence of sulfonamide in combination with methoxy substitution enhanced DNA fragmentation and there by acting as effective derivative for Hepatocellular carcinoma.</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><doi>10.1007/s42452-020-03726-7</doi><oa>free_for_read</oa></addata></record> |
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| subjects | Anticancer properties Antitumor activity Apoptosis Applied and Technical Physics Benzothiazole Cancer therapies Carbon Chemistry/Food Science Chemistry: Pharmaceutical DNA fragmentation Drug dosages Earth Sciences Engineering Environment Hepatocellular carcinoma Hepatocytes Hypoxia Liver cancer Materials Science Medical Medicinal and Clinical Chemistry Melanoma Radiation Radiosensitizers Research Article Sulfonamides |
| title | Studies on imidazo[2,1-b][1,3]benzothiazole derivatives as new radiosensitizers |
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