Synthesis, in vitro and in vivo antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives
A novel series of 5-nitro-1H-benzimidazole derivatives substituted at position 1 by heterocyclic rings was synthesized. Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no ac...
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| Veröffentlicht in: | Journal of enzyme inhibition and medicinal chemistry 2015-09, Vol.30 (5), p.826-845 |
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| container_title | Journal of enzyme inhibition and medicinal chemistry |
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| creator | Shaker, Yasser M. Omar, Mohamed A. Mahmoud, Khaled Elhallouty, Salwa M. El-Senousy, Waled M. Ali, Mamdouh M. Mahmoud, Abeer E. Abdel-Halim, Abeer H. Soliman, Saeed M. El Diwani, Hoda I. |
| description | A novel series of 5-nitro-1H-benzimidazole derivatives substituted at position 1 by heterocyclic rings was synthesized. Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain. |
| doi_str_mv | 10.3109/14756366.2014.979344 |
| format | Article |
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Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain.</description><identifier>ISSN: 1475-6366</identifier><identifier>EISSN: 1475-6374</identifier><identifier>DOI: 10.3109/14756366.2014.979344</identifier><identifier>PMID: 25567722</identifier><language>eng</language><publisher>England: Informa Healthcare</publisher><subject>Animals ; Antineoplastic Agents - chemical synthesis ; Antineoplastic Agents - chemistry ; Antineoplastic Agents - pharmacology ; Antitumor ; antiviral ; Antiviral Agents - chemical synthesis ; Antiviral Agents - chemistry ; Antiviral Agents - pharmacology ; benzimidazoles ; Benzimidazoles - chemical synthesis ; Benzimidazoles - chemistry ; Benzimidazoles - pharmacology ; Cell Line, Tumor ; Cell Proliferation - drug effects ; Cell Survival - drug effects ; cytotoxicity ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Microbial Sensitivity Tests ; Molecular Structure ; Neoplasms, Experimental - drug therapy ; Neoplasms, Experimental - pathology ; Rats ; Rotavirus - drug effects ; Structure-Activity Relationship</subject><ispartof>Journal of enzyme inhibition and medicinal chemistry, 2015-09, Vol.30 (5), p.826-845</ispartof><rights>2015 Informa UK Ltd. 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Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain.</description><subject>Animals</subject><subject>Antineoplastic Agents - chemical synthesis</subject><subject>Antineoplastic Agents - chemistry</subject><subject>Antineoplastic Agents - pharmacology</subject><subject>Antitumor</subject><subject>antiviral</subject><subject>Antiviral Agents - chemical synthesis</subject><subject>Antiviral Agents - chemistry</subject><subject>Antiviral Agents - pharmacology</subject><subject>benzimidazoles</subject><subject>Benzimidazoles - chemical synthesis</subject><subject>Benzimidazoles - chemistry</subject><subject>Benzimidazoles - pharmacology</subject><subject>Cell Line, Tumor</subject><subject>Cell Proliferation - drug effects</subject><subject>Cell Survival - drug effects</subject><subject>cytotoxicity</subject><subject>Dose-Response Relationship, Drug</subject><subject>Drug Screening Assays, Antitumor</subject><subject>Humans</subject><subject>Microbial Sensitivity Tests</subject><subject>Molecular Structure</subject><subject>Neoplasms, Experimental - drug therapy</subject><subject>Neoplasms, Experimental - pathology</subject><subject>Rats</subject><subject>Rotavirus - drug effects</subject><subject>Structure-Activity Relationship</subject><issn>1475-6366</issn><issn>1475-6374</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtOwzAQRS0EoqXwBwj5A0jxK3ayQqjiJVViAawjxw9hlMTFdoPar6chtEtWc-fq3hnpAHCJ0ZxiVN5gJnJOOZ8ThNm8FCVl7AhMBzvjVLDjg-Z8As5i_ESIYILZKZiQPOdCEDIFX6-bLn2Y6OI1dB3sXQoeyk6PSz_o5NK69eHXHbbeBdlAqQaVNtBb2PneNBBncV3HIZ2MhrXptq51Wm59Y6A2wfVy1zDxHJxY2URz8Tdn4P3h_m3xlC1fHp8Xd8tMUU5TVgiWW2Qxl7o0Mi81l5YTXBDCjapzURSFNQVFZa4VEgIRzUhJay2VtkgpSWeAjXdV8DEGY6tVcK0MmwqjaiBY7QlWA8FqJLirXY211bpujT6U9sh2gdsx4DrrQyu_fWh0leSm8cEG2SkXh_P_vPgBMxCC1w</recordid><startdate>20150903</startdate><enddate>20150903</enddate><creator>Shaker, Yasser M.</creator><creator>Omar, Mohamed A.</creator><creator>Mahmoud, Khaled</creator><creator>Elhallouty, Salwa M.</creator><creator>El-Senousy, Waled M.</creator><creator>Ali, Mamdouh M.</creator><creator>Mahmoud, Abeer E.</creator><creator>Abdel-Halim, Abeer H.</creator><creator>Soliman, Saeed M.</creator><creator>El Diwani, Hoda I.</creator><general>Informa Healthcare</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></search><sort><creationdate>20150903</creationdate><title>Synthesis, in vitro and in vivo antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives</title><author>Shaker, Yasser M. ; 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Cytotoxicity and antiviral activity of the new compounds were tested. Compound 3 was more active than doxorubicin against A-549, HCT-116 and MCF-7. However, compound 3 showed no activity against human liver carcinoma Hep G-2 cell line. Compounds 9 and 17b (E) showed potency near to doxorubicin against the four cell lines. The acute toxicity of compound 9 on liver cancer induced in rats was determined in vivo. Interestingly, it showed restoration activity of liver function and pathology towards normal as compared to the cancer-bearing rats induced by DENA. Compounds 17a (Z), 17b (E) and 18a (Z) were the most promising compounds for their antiviral activity against rotavirus Wa strain.</abstract><cop>England</cop><pub>Informa Healthcare</pub><pmid>25567722</pmid><doi>10.3109/14756366.2014.979344</doi><tpages>20</tpages></addata></record> |
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| subjects | Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Antitumor antiviral Antiviral Agents - chemical synthesis Antiviral Agents - chemistry Antiviral Agents - pharmacology benzimidazoles Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Cell Survival - drug effects cytotoxicity Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Humans Microbial Sensitivity Tests Molecular Structure Neoplasms, Experimental - drug therapy Neoplasms, Experimental - pathology Rats Rotavirus - drug effects Structure-Activity Relationship |
| title | Synthesis, in vitro and in vivo antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives |
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