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Synthesis of novel carbazole hydrazine-carbothioamide scaffold as potent antioxidant, anticancer and antimicrobial agents

İrfan ÇapanDepartment of Pharmaceutical Basic Sciences, Faculty of Pharmacy, Gazi University, 06330, Ankara, Türkiye. [email protected]Mohammed HawashDepartment of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine. [email protected]Mohammed T. QaoudDepartment of Pharmacy, Faculty of Pharmacy, Cyprus International University, Northern Cyprus, Mersin 10, 99258, Nicosia, TürkiyeLevent GülümDepartment of Plant and Animal Production, Mudurnu Süreyya Astarcı Vocational College, Bolu Abant İzzet Baysal University, Bolu, TürkiyeEzgi Nurdan Yenilmez TunoğluDepartment of Medical Laboratory Techniques, Vocational School of Health Services, Demiroğlu Bilim University, Istanbul, TürkiyeKezban Uçar ÇifciDepartment of Molecular Medicine, Faculty of Health Sciences, University of Health Sciences, Istanbul, TürkiyeBekir Sıtkı ÇevrimliDepartment of Chemistry and Chemical Processing Technologies, Technical Sciences Vocational College, Gazi University, Ankara, TürkiyeYusuf SertSorgun Vocational College, Yozgat Bozok University, Yozgat, TürkiyeSüleyman ServiDepartment of Chemistry, Faculty of Science, Fırat University, Elazığ, Türkiyeİrfan KocaDepartment of Chemistry, Faculty of Art & Sciences, Yozgat Bozok University, Yozgat, TürkiyeYusuf TutarFaculty of Pharmacy, Division of Biochemistry, University of Health Sciences, Istanbul, Türkiye

2024en

ABI

Annotatsiya

BACKGROUND: Carbazole-based molecules containing thiosemicarbazide functional groups are recognized for their diverse biological activities, particularly in enhancing therapeutic anticancer effects through inhibiting crucial pathways. These derivatives also exhibit noteworthy antioxidant properties. OBJECTIVES: This study aims to synthesize, characterize, and evaluate the antioxidant and anticancer activities of 18 novel carbazole derivatives. METHODS: The radical scavenging capabilities of the compounds were assessed using the 2,2-diphenyl-1-picrylhydrazyl assay. Antiproliferative activities were evaluated on MCF-7 cancer cell lines through viability assays. Additionally, the modulation of the PI3K/Akt/mTOR pathway, apoptosis/necrosis induction, and cell cycle analysis were conducted for the most promising anticancer agents. RESULTS: values of 2.02 and 4.99 µM, respectively. Compound 4o, in particular, exhibited promising activity by targeting the PI3K/Akt/mTOR signaling pathway, inhibiting tumor survival, inducing apoptosis, and causing cell cycle arrest in MCF-7 cell lines. Furthermore, compound 4o was showed significant antimicrobial activities against S. aureus and E. coli, and antifungal effect against C. albicans. Its potential to overcome drug resistance through this pathway inhibition highlights its promise as an anticancer agent. Molecular docking simulations supported these findings, revealing favorable binding profiles and interactions within the active sites of the enzymes PI3K, AKT1, and mTOR. Moreover, assessing the druggability of the newly synthesized thiosemicarbazide derivatives demonstrated optimal physicochemical properties, further endorsing their potential as drug candidates.

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DOI: 10.1186/s13065-024-01207-1

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