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Information Journal Paper

Title

Design, Synthesis and Biological Evaluation of4-(Imidazolylmethyl)-2-(4-methylsulfonyl phenyl)-Quinoline Derivatives as Selective COX-2 Inhibitors and In-vitro Anti-breast Cancer Agents

Pages

  169-177

Abstract

 A new group of 4-(Imidazolylmethyl)quinoline derivatives possessing a methylsulfonyl COX-2 pharmacophore at the para position of the C-2 phenyl ring were designed and synthesized as selective COX-2 inhibitors and in-vitroanti Breast cancer agents. In-vitro COX-1 and COX-2 inhibition studies showed that all the compounds were potent and selective inhibitors of the COX-2 isozyme with IC50 values in the potent range 0. 063-0. 090 μ M, and COX-2 selectivity indexes in the 179. 9 to 547. 6 range. Molecular modeling studies indicated that the methylsulfonyl substituent can be inserted into the secondary pocket of COX-2 active site for interactions with Arg513. Cytotoxicity of Quinolines 9a-e against human Breast cancer MCF-7 and T47D cell lines were also evaluated. All the compounds 9a-e were more cytotoxic against MCF-7 cells in comparison with those of T47D which express aromatase mRNA less than MCF-7 cells. The data showed that the increase of lipophilic properties of substituents on the C-7 and C-8 quinoline ring increased their cytotoxicity on MCF-7cells andCOX-2 inhibitory activity. Among the Quinolines 9a-e, 4-((1H-Imidazol-1-yl)methyl) 7, 8, 9, 10-tetrahydro-2-(4-methylsulfonylphenyl)-benzo[h]quinoline (9d)was identified as the most potent andselective COX-2inhibitor as well as the most cytotoxic agent against MCF-7 cells.

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    • Cite

    APA: Copy

    GHODSI, RAZIEH, AZIZI, EBRAHIM, & ZARGHI, AFSHIN. (2016). Design, Synthesis and Biological Evaluation of4-(Imidazolylmethyl)-2-(4-methylsulfonyl phenyl)-Quinoline Derivatives as Selective COX-2 Inhibitors and In-vitro Anti-breast Cancer Agents. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 15(1), 169-177. SID. https://sid.ir/paper/288559/en

    Vancouver: Copy

    GHODSI RAZIEH, AZIZI EBRAHIM, ZARGHI AFSHIN. Design, Synthesis and Biological Evaluation of4-(Imidazolylmethyl)-2-(4-methylsulfonyl phenyl)-Quinoline Derivatives as Selective COX-2 Inhibitors and In-vitro Anti-breast Cancer Agents. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2016;15(1):169-177. Available from: https://sid.ir/paper/288559/en

    IEEE: Copy

    RAZIEH GHODSI, EBRAHIM AZIZI, and AFSHIN ZARGHI, “Design, Synthesis and Biological Evaluation of4-(Imidazolylmethyl)-2-(4-methylsulfonyl phenyl)-Quinoline Derivatives as Selective COX-2 Inhibitors and In-vitro Anti-breast Cancer Agents,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 15, no. 1, pp. 169–177, 2016, [Online]. Available: https://sid.ir/paper/288559/en

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