Abstract
A new series of 3',4'-bis(3,4,5-trimethoxyphenyl)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one derivatives was designed and synthesized. The cytotoxic effects of the synthesized compounds were evaluated on several different human cancer cells. Among them, compound 9e displayed the most potent in vitro antiproliferative activity with IC50 values of 0.07±0.01 µM on T47D cells. Another potent derivative 9h displayed an IC50 value of 0.12±0.07 µM against T47D cells, comparable to that of the positive controls (Colchicine Cisplatin Vincristine Vinblastine Doxorubicin Celecoxib). The structure-activity relationships were discussed and both anti-tubulin and COX-2 inhibitory effects were proposed for the developed compounds.
Keywords: Antitubulin, COX-2 inhibitor, 1, 3-dipolar cycloaddition, hybrid compounds, MTT assay, spiro-isoxazoline.
Letters in Drug Design & Discovery
Title:Design, Synthesis and in vitro Cytotoxicity Evaluation of New 3',4'-bis (3,4,5-trisubstituted)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one Derivatives as Promising Anticancer Agents
Volume: 11 Issue: 10
Author(s): Hoda Abolhasani, Afshin Zarghi, Ahmad Abolhasani, Maryam Hamzeh-Mivehroud, Nasrin Bargahi, Behrouz Notash, Javid Shahbazi Mojarrad and Siavoush Dastmalchi
Affiliation:
Keywords: Antitubulin, COX-2 inhibitor, 1, 3-dipolar cycloaddition, hybrid compounds, MTT assay, spiro-isoxazoline.
Abstract: A new series of 3',4'-bis(3,4,5-trimethoxyphenyl)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one derivatives was designed and synthesized. The cytotoxic effects of the synthesized compounds were evaluated on several different human cancer cells. Among them, compound 9e displayed the most potent in vitro antiproliferative activity with IC50 values of 0.07±0.01 µM on T47D cells. Another potent derivative 9h displayed an IC50 value of 0.12±0.07 µM against T47D cells, comparable to that of the positive controls (Colchicine Cisplatin Vincristine Vinblastine Doxorubicin Celecoxib). The structure-activity relationships were discussed and both anti-tubulin and COX-2 inhibitory effects were proposed for the developed compounds.
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Abolhasani Hoda, Zarghi Afshin, Abolhasani Ahmad, Hamzeh-Mivehroud Maryam, Bargahi Nasrin, Notash Behrouz, Mojarrad Shahbazi Javid and Dastmalchi Siavoush, Design, Synthesis and in vitro Cytotoxicity Evaluation of New 3',4'-bis (3,4,5-trisubstituted)-4'H-spiro[indene-2,5'-isoxazol]-1(3H)-one Derivatives as Promising Anticancer Agents, Letters in Drug Design & Discovery 2014; 11 (10) . https://dx.doi.org/10.2174/1570180811666140704172442
DOI https://dx.doi.org/10.2174/1570180811666140704172442 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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