Novel dermacozine-1-carboxamides as promising anticancer agents with tubulin polymerization inhibitory activity |
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| Authors: | Venkata Rao Ghanta Nagaraju Madala Aparna Pasula Sai Kiran S S Pindiprolu Kumara Swamy Battula Praveen T Krishnamurthy Balamurali Raman |
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| Institution: | GVK Biosciences Private Limited, Medicinal Chemistry Division, 28 A, IDA Nacharam, Hyderabad Telangana India.; Department of Chemistry, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad Telangana India ; Department of Pharmacology, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, Tamil Nadu India.; Department of Chemistry, Kakatiya University, Warangal-506 009 Telangana India |
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| 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.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). |
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