Novel dermacozine-1-carboxamides as promising anticancer agents with tubulin polymerization inhibitory activity

新型德马津-1-甲酰胺是一种具有微管蛋白聚合抑制活性的有前途的抗癌药物

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作者:Venkata Rao Ghanta, Nagaraju Madala, Aparna Pasula, Sai Kiran S S Pindiprolu, Kumara Swamy Battula, Praveen T Krishnamurthy, Balamurali Raman

Abstract

In the present study, novel dermacozine-1-carboxamides (8a-8n) were synthesized and screened for their in vitro cytotoxic activity against three different cancer cell lines: MCF-7 (breast cancer), A-549 (lung cancer) and DU145 (prostate cancer). All the compounds showed more efficiency against the DU145 cell line than against the MCF-7 and A-549 cell lines. Furthermore, 8a (CTC50: 7.02 μM) and 8l (CTC50: 6.32 μM) have been found to be more effective against the DU145 cells as they arrest the cell cycle at the G2/M phase by interfering with tubulin polymerization; these results indicate that these compounds act as potential anti-cancer agents by inhibiting tubulin polymerization.

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