Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice
[Display omitted] Cancer is a leading cause of death in developed countries and second cause in developing countries. Herein we are reporting the synthesis of novel bisbenzimidazole derivatives and their anticancer properties. Among the newly synthesized bisbenzimidazoles, 3-(4-flurophenylsulfonyl)-...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2015-06, Vol.25 (12), p.2589-2593 |
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| creator | Roopashree, Rangaswamy Mohan, Chakrabhavi Dhananjaya Swaroop, Toreshettahally Ramesh Jagadish, Swamy Raghava, Byregowda Balaji, Kyathegowdanadoddi Srinivas Jayarama, Shankar Basappa Rangappa, Kanchugarakoppal Subbegowda |
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Cancer is a leading cause of death in developed countries and second cause in developing countries. Herein we are reporting the synthesis of novel bisbenzimidazole derivatives and their anticancer properties. Among the newly synthesized bisbenzimidazoles, 3-(4-flurophenylsulfonyl)-1,7-dimethyl-2-propyl-1H,3H-2,5-bibenzo[d]imidazole (FDPB) presented as a potent antiproliferative agent against HeLa, HCT116 and A549 cells with selectivity over normal Vero cells (IC50 >50μM). Additionally, we evaluated the efficacy of lead compound against Ehrlich ascites tumor (EAT) bearing mice for its antitumor and antiangiogenic properties. Our lead compound significantly reduced the cell viability, body weight, ascites volume and downregulated the formation of neovasculature and production of Vascular Endothelial Growth Factor (VEGF). |
| doi_str_mv | 10.1016/j.bmcl.2015.04.010 |
| format | Article |
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Cancer is a leading cause of death in developed countries and second cause in developing countries. Herein we are reporting the synthesis of novel bisbenzimidazole derivatives and their anticancer properties. Among the newly synthesized bisbenzimidazoles, 3-(4-flurophenylsulfonyl)-1,7-dimethyl-2-propyl-1H,3H-2,5-bibenzo[d]imidazole (FDPB) presented as a potent antiproliferative agent against HeLa, HCT116 and A549 cells with selectivity over normal Vero cells (IC50 >50μM). Additionally, we evaluated the efficacy of lead compound against Ehrlich ascites tumor (EAT) bearing mice for its antitumor and antiangiogenic properties. Our lead compound significantly reduced the cell viability, body weight, ascites volume and downregulated the formation of neovasculature and production of Vascular Endothelial Growth Factor (VEGF).</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2015.04.010</identifier><identifier>PMID: 25920563</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Angiogenesis ; Angiogenesis Inhibitors - chemical synthesis ; Angiogenesis Inhibitors - pharmacology ; Angiogenesis Inhibitors - therapeutic use ; Animals ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - pharmacology ; Antineoplastic Agents - therapeutic use ; Antiproliferative ; Ascites ; Bisbenzimidazole ; Bisbenzimidazole - chemistry ; Bisbenzimidazole - pharmacology ; Bisbenzimidazole - therapeutic use ; Body Weight - drug effects ; Carcinoma, Ehrlich Tumor - drug therapy ; Cell Line, Tumor ; Cell Proliferation - drug effects ; Cell Survival - drug effects ; Cercopithecus aethiops ; Down-Regulation - drug effects ; Ehrlich ascites tumor ; HCT116 Cells ; HeLa Cells ; Humans ; Mice ; Micro vessel density ; Vascular Endothelial Growth Factor ; Vascular Endothelial Growth Factor A - metabolism ; Vero Cells</subject><ispartof>Bioorganic & medicinal chemistry letters, 2015-06, Vol.25 (12), p.2589-2593</ispartof><rights>2015 Elsevier Ltd</rights><rights>Copyright © 2015 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c470t-17e99797c44a28c4dacb44d24e4f0a332b1f1521250229a777cdd949f7beb6523</citedby><cites>FETCH-LOGICAL-c470t-17e99797c44a28c4dacb44d24e4f0a332b1f1521250229a777cdd949f7beb6523</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2015.04.010$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25920563$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Roopashree, Rangaswamy</creatorcontrib><creatorcontrib>Mohan, Chakrabhavi Dhananjaya</creatorcontrib><creatorcontrib>Swaroop, Toreshettahally Ramesh</creatorcontrib><creatorcontrib>Jagadish, Swamy</creatorcontrib><creatorcontrib>Raghava, Byregowda</creatorcontrib><creatorcontrib>Balaji, Kyathegowdanadoddi Srinivas</creatorcontrib><creatorcontrib>Jayarama, Shankar</creatorcontrib><creatorcontrib>Basappa</creatorcontrib><creatorcontrib>Rangappa, Kanchugarakoppal Subbegowda</creatorcontrib><title>Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Cancer is a leading cause of death in developed countries and second cause in developing countries. Herein we are reporting the synthesis of novel bisbenzimidazole derivatives and their anticancer properties. Among the newly synthesized bisbenzimidazoles, 3-(4-flurophenylsulfonyl)-1,7-dimethyl-2-propyl-1H,3H-2,5-bibenzo[d]imidazole (FDPB) presented as a potent antiproliferative agent against HeLa, HCT116 and A549 cells with selectivity over normal Vero cells (IC50 >50μM). Additionally, we evaluated the efficacy of lead compound against Ehrlich ascites tumor (EAT) bearing mice for its antitumor and antiangiogenic properties. Our lead compound significantly reduced the cell viability, body weight, ascites volume and downregulated the formation of neovasculature and production of Vascular Endothelial Growth Factor (VEGF).</description><subject>Angiogenesis</subject><subject>Angiogenesis Inhibitors - chemical synthesis</subject><subject>Angiogenesis Inhibitors - pharmacology</subject><subject>Angiogenesis Inhibitors - therapeutic use</subject><subject>Animals</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Antineoplastic Agents - therapeutic use</subject><subject>Antiproliferative</subject><subject>Ascites</subject><subject>Bisbenzimidazole</subject><subject>Bisbenzimidazole - chemistry</subject><subject>Bisbenzimidazole - pharmacology</subject><subject>Bisbenzimidazole - therapeutic use</subject><subject>Body Weight - drug effects</subject><subject>Carcinoma, Ehrlich Tumor - drug therapy</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Cell Survival - drug effects</subject><subject>Cercopithecus aethiops</subject><subject>Down-Regulation - drug effects</subject><subject>Ehrlich ascites tumor</subject><subject>HCT116 Cells</subject><subject>HeLa Cells</subject><subject>Humans</subject><subject>Mice</subject><subject>Micro vessel density</subject><subject>Vascular Endothelial Growth Factor</subject><subject>Vascular Endothelial Growth Factor A - metabolism</subject><subject>Vero Cells</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kDtvFDEURi0EIkvgD1AglzQzXHuux2uJBkXhIUXQgERn-XFn16t5BNsbKfn1mdUGSqrbnO9I9zD2VkArQPQfDq2fwthKEKoFbEHAM7YR2GPTIajnbAOmh2Zr8PcFe1XKAUAgIL5kF1IZCarvNix-X-5o5OV-rnuqKXCfiqf5IU0puodlJF73rvLq8o5q4W7epWVHM5VUeJr59T6PKey5KyFVKjy4HNK8TI57cjnNOz6lQK_Zi8GNhd483Uv26_P1z6uvzc2PL9-uPt00ATXURmgyRhsdEJ3cBowueMQokXAA13XSi0EoKaQCKY3TWocYDZpBe_K9kt0le3_23ublz5FKtVMqgcbRzbQcixX9tuuU0kasqDyjIS-lZBrsbU6Ty_dWgD3VtQd7qmtPdS2gXeuuo3dP_qOfKP6b_M25Ah_PAK1f3iXKdu1Cc6CYMoVq45L-538E7QaMiw</recordid><startdate>20150615</startdate><enddate>20150615</enddate><creator>Roopashree, Rangaswamy</creator><creator>Mohan, Chakrabhavi Dhananjaya</creator><creator>Swaroop, Toreshettahally Ramesh</creator><creator>Jagadish, Swamy</creator><creator>Raghava, Byregowda</creator><creator>Balaji, Kyathegowdanadoddi Srinivas</creator><creator>Jayarama, Shankar</creator><creator>Basappa</creator><creator>Rangappa, Kanchugarakoppal Subbegowda</creator><general>Elsevier Ltd</general><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>7X8</scope></search><sort><creationdate>20150615</creationdate><title>Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice</title><author>Roopashree, Rangaswamy ; Mohan, Chakrabhavi Dhananjaya ; Swaroop, Toreshettahally Ramesh ; Jagadish, Swamy ; Raghava, Byregowda ; Balaji, Kyathegowdanadoddi Srinivas ; Jayarama, Shankar ; Basappa ; Rangappa, Kanchugarakoppal Subbegowda</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c470t-17e99797c44a28c4dacb44d24e4f0a332b1f1521250229a777cdd949f7beb6523</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Angiogenesis</topic><topic>Angiogenesis Inhibitors - chemical synthesis</topic><topic>Angiogenesis Inhibitors - pharmacology</topic><topic>Angiogenesis Inhibitors - therapeutic use</topic><topic>Animals</topic><topic>Antineoplastic Agents - chemical synthesis</topic><topic>Antineoplastic Agents - pharmacology</topic><topic>Antineoplastic Agents - therapeutic use</topic><topic>Antiproliferative</topic><topic>Ascites</topic><topic>Bisbenzimidazole</topic><topic>Bisbenzimidazole - chemistry</topic><topic>Bisbenzimidazole - pharmacology</topic><topic>Bisbenzimidazole - therapeutic use</topic><topic>Body Weight - drug effects</topic><topic>Carcinoma, Ehrlich Tumor - drug therapy</topic><topic>Cell Line, Tumor</topic><topic>Cell Proliferation - drug effects</topic><topic>Cell Survival - drug effects</topic><topic>Cercopithecus aethiops</topic><topic>Down-Regulation - drug effects</topic><topic>Ehrlich ascites tumor</topic><topic>HCT116 Cells</topic><topic>HeLa Cells</topic><topic>Humans</topic><topic>Mice</topic><topic>Micro vessel density</topic><topic>Vascular Endothelial Growth Factor</topic><topic>Vascular Endothelial Growth Factor A - metabolism</topic><topic>Vero Cells</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Roopashree, Rangaswamy</creatorcontrib><creatorcontrib>Mohan, Chakrabhavi Dhananjaya</creatorcontrib><creatorcontrib>Swaroop, Toreshettahally Ramesh</creatorcontrib><creatorcontrib>Jagadish, Swamy</creatorcontrib><creatorcontrib>Raghava, Byregowda</creatorcontrib><creatorcontrib>Balaji, Kyathegowdanadoddi Srinivas</creatorcontrib><creatorcontrib>Jayarama, Shankar</creatorcontrib><creatorcontrib>Basappa</creatorcontrib><creatorcontrib>Rangappa, Kanchugarakoppal Subbegowda</creatorcontrib><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><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Roopashree, Rangaswamy</au><au>Mohan, Chakrabhavi Dhananjaya</au><au>Swaroop, Toreshettahally Ramesh</au><au>Jagadish, Swamy</au><au>Raghava, Byregowda</au><au>Balaji, Kyathegowdanadoddi Srinivas</au><au>Jayarama, Shankar</au><au>Basappa</au><au>Rangappa, Kanchugarakoppal Subbegowda</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2015-06-15</date><risdate>2015</risdate><volume>25</volume><issue>12</issue><spage>2589</spage><epage>2593</epage><pages>2589-2593</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Cancer is a leading cause of death in developed countries and second cause in developing countries. Herein we are reporting the synthesis of novel bisbenzimidazole derivatives and their anticancer properties. Among the newly synthesized bisbenzimidazoles, 3-(4-flurophenylsulfonyl)-1,7-dimethyl-2-propyl-1H,3H-2,5-bibenzo[d]imidazole (FDPB) presented as a potent antiproliferative agent against HeLa, HCT116 and A549 cells with selectivity over normal Vero cells (IC50 >50μM). Additionally, we evaluated the efficacy of lead compound against Ehrlich ascites tumor (EAT) bearing mice for its antitumor and antiangiogenic properties. Our lead compound significantly reduced the cell viability, body weight, ascites volume and downregulated the formation of neovasculature and production of Vascular Endothelial Growth Factor (VEGF).</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>25920563</pmid><doi>10.1016/j.bmcl.2015.04.010</doi><tpages>5</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2015-06, Vol.25 (12), p.2589-2593 |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Angiogenesis Angiogenesis Inhibitors - chemical synthesis Angiogenesis Inhibitors - pharmacology Angiogenesis Inhibitors - therapeutic use Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Antiproliferative Ascites Bisbenzimidazole Bisbenzimidazole - chemistry Bisbenzimidazole - pharmacology Bisbenzimidazole - therapeutic use Body Weight - drug effects Carcinoma, Ehrlich Tumor - drug therapy Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects Cercopithecus aethiops Down-Regulation - drug effects Ehrlich ascites tumor HCT116 Cells HeLa Cells Humans Mice Micro vessel density Vascular Endothelial Growth Factor Vascular Endothelial Growth Factor A - metabolism Vero Cells |
| title | Novel synthetic bisbenzimidazole that targets angiogenesis in Ehrlich ascites carcinoma bearing mice |
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