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

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.

Cite this article as:

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