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Novel HDAC/Tubulin Dual Inhibitor: Design, Synthesis and Docking Studies of ?-Phthalimido-Chalcone Hybrids as Potential Anticancer Agents with Apoptosis-Inducing Activity.

ABSTRACT: Introduction:In order to develop novel anticancer HDAC/tubulin dual inhibitors, a novel series of ?-phthalimido-substituted chalcones-based hybrids was synthesized and characterized by IR, 1H NMR, 13C NMR, mass spectroscopy and X-ray analysis. Methods:All the synthesized compounds were evaluated for their in vitro anticancer activity against MCF-7 and HepG2 human cancer cell lines using MTT assay. To explore the mechanism of action of the synthesized compounds, in vitro ?-tubulin polymerization and HDAC 1 and 2 inhibitory activity were measured for the most potent anticancer hybrids. Further, cell cycle analysis was also evaluated. Results:The trimethoxy derivative 7j showed the most potent anticancer activity, possessed the most potent ?-tubulin polymerase and HDAC 1 and 2 inhibitory activity and efficiently induced cell cycle arrest at both G2/M and preG1phases in the MCF-7 cell line.

SUBMITTER: Mourad AAE 

PROVIDER: S-EPMC7425103 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature

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Novel HDAC/Tubulin Dual Inhibitor: Design, Synthesis and Docking Studies of α-Phthalimido-Chalcone Hybrids as Potential Anticancer Agents with Apoptosis-Inducing Activity.

Mourad Ahmed A E AAE   Mourad Mai A E MAE   Jones Peter G PG  

Drug design, development and therapy 20200803

<h4>Introduction</h4>In order to develop novel anticancer HDAC/tubulin dual inhibitors, a novel series of α-phthalimido-substituted chalcones-based hybrids was synthesized and characterized by IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR, mass spectroscopy and X-ray analysis.<h4>Methods</h4>All the synthesized compounds were evaluated for their in vitro anticancer activity against MCF-7 and HepG2 human cancer cell lines using MTT assay. To explore the mechanism of action of the synthesized compound  ...[more]

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