Abstract
As a continuation to our previous work in developing anticancer agents, eighteen symmetrical biphenyl derivatives structurally related to taspine were synthesized and evaluated in vitro and in vivo. All the compounds were prepared with varied substitutions in the phenyl ring of aniline moiety. The cytotoxicity and anticancer activity of biphenyls was evaluated against various human tumor and normal cell line. Antiproliferative assays indicated that some of them exhibited potent anticancer activity. The potent antiproliferative activity of these compounds against ECV304 suggested that these biphenyls could be served as antiangiogenic agents. The highly active compound (2) also exhibited potent growth inhibition against cancer cell lines in vivo. Our findings demonstrated that these symmetrical biphenyl derivatives would be a promising candidate as novel anticancer agents.
Keywords: Symmetrical biphenyls, Antiproliferative activity, Cytotoxicity, Antitumor agents, VEGFR-2, antiangiogenic agents, Antiproliferative, biphenyls, Antitumor, Chemotherapy
Medicinal Chemistry
Title:Facile Synthesis and Biological Evaluation of Novel Symmetrical Biphenyls as Antitumor Agents
Volume: 8 Issue: 2
Author(s): Jie Zhang, Yanmin Zhang, Xiaoyan Pan, Chen Wang, Zhigang Hu, Sicen Wang, Langchong He
Affiliation:
Keywords: Symmetrical biphenyls, Antiproliferative activity, Cytotoxicity, Antitumor agents, VEGFR-2, antiangiogenic agents, Antiproliferative, biphenyls, Antitumor, Chemotherapy
Abstract: As a continuation to our previous work in developing anticancer agents, eighteen symmetrical biphenyl derivatives structurally related to taspine were synthesized and evaluated in vitro and in vivo. All the compounds were prepared with varied substitutions in the phenyl ring of aniline moiety. The cytotoxicity and anticancer activity of biphenyls was evaluated against various human tumor and normal cell line. Antiproliferative assays indicated that some of them exhibited potent anticancer activity. The potent antiproliferative activity of these compounds against ECV304 suggested that these biphenyls could be served as antiangiogenic agents. The highly active compound (2) also exhibited potent growth inhibition against cancer cell lines in vivo. Our findings demonstrated that these symmetrical biphenyl derivatives would be a promising candidate as novel anticancer agents.
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Cite this article as:
Jie Zhang, Yanmin Zhang, Xiaoyan Pan, Chen Wang, Zhigang Hu, Sicen Wang, Langchong He , Facile Synthesis and Biological Evaluation of Novel Symmetrical Biphenyls as Antitumor Agents, Medicinal Chemistry 2012; 8 (2) . https://dx.doi.org/10.2174/157340612800493656
DOI https://dx.doi.org/10.2174/157340612800493656 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
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