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Document Type |
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Project |
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Document Title |
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Synthesis and Biological Evaluation of Some New Substituted Fused Pyrazole Ring Systems as Anticancer and Antimicrobial agents. تشييد بعض حلقات البيرازول المدمجة الجديدة و المستبدلة و تقييم فعاليتها البيولوجية كمضادات للسرطان و مضادات للميكروبات. |
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Subject |
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Synthesis and Biological Evaluation of Some New Substituted Fused Pyrazole Ring Systems as Anticancer and Antimicrobial agents. |
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Document Language |
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Arabic |
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Abstract |
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Cancer is a growing public problem whose estimated worldwide new incidence is about 6 million cases per year. It is the second major cause of death after cardiovascular diseases and is characterized by unregulated proliferation of cells. Therefore, such rapid spread of cancer has stimulated an unprecedented level of medicinal chemistry research activity directed towards the search for new structure leads that may be of use in designing novel antitumor drugs.
On the other hand, infections caused by multi-drug resistant pathogenic microorganisms pose a serious challenge to the medical community and the need for an effective therapy has led to a search for novel antibacterial agents. Among the wide variety of heterocycles that have been explored for developing potential pharmacologically active compounds, pyrazoles fused with different heterocycles that are known to contribute to various chemotherapeutic effects have emerged as antimicrobial, antiviral and anticancer agents. Moreover, pyrones and their pyridine analogs are well known for their various potential chemotherapeutic activities. Prompted by these facts, and in continuation of our search for new potentially active chemotherapeutic agents, it was proposed to synthesize and investigate the anticancer and antimicrobial activities of some new polysubstiuted fused heterocyclic ring systems namely; pyrano[4,3-c]pyrazoles and pyrazolo[4,3-c]pyridines. The targeted compounds where designed so as to hybridize the pyrazole ring with the pyrone and/or pyridine moieties, respectively, hoping to obtain synergistic anticancer and/or antimicrobial activities. The substitution pattern of the target compounds include various functionalities such as the amino, derived imine, ureido, thioureido and sulfonamido groups that are reported to contribute to various chemotherapeutic activities. The variation in the nature and size of substituents at such functionalities was thought to be of interest as it would offer variable electronic, lipophilic and steric environment that would influence the targeted biological activities. This combination is suggested in an attempt to investigate the influence of such hybridization on the anticipated anticancer and/or antimicrobial activity. The structures of the newly synthesized compounds will be confirmed with elementary microanalyses and substantiated with IR and 1H-NMR data. The target compounds will be subjected to the National Cancer Institute NCI in vitro disease-oriented human cells screening panel assay, Maryland, USA, to screen their anticancer activity. In addition, the in vitro antibacterial and antifungal activities of the target compounds will be also determined. |
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Publishing Year |
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1428 AH
2007 AD |
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Added Date |
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Tuesday, June 29, 2010 |
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Researchers
| محمد صادر الصاعدي | Al-Saadi, Mohammed Sader | Investigator | Doctorate | |
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