Chemical Biology and Drug Design
Chemical Biology and Drug Design
5 years ago

Novel Menadione Hybrids: Synthesis, anticancer activity and cell based studies

Novel Menadione Hybrids: Synthesis, anticancer activity and cell based studies
Sistla Ramakrishna, Vadithe Lakshma Nayak, Uppuluri Venkata Mallavadhani, Chakka Vara Prasad
A series of novel menadione based triazole hybrids were designed and synthesized by employing copper catalyzed azide-alkyne cycloaddition (CuAAC). All the synthesized hybrids were characterized by their spectral data (1H NMR, 13C NMR, IR and HRMS). The synthesized compounds were evaluated for their anticancer activity against five selected cancer cell lines including lung (A549), prostate (DU-145), cervical (Hela), breast (MCF-7) and mouse melanoma (B-16) by using MTT assay. The screening results showed that majority of the synthesized compounds displayed significant anticancer activity. Among the tested compounds, the triazoles 5 and 6 exhibited potent activity against all cell lines. In particular, compound 6 showed higher potency than the standard tamoxifen and parent menadione against MCF-7 cell line. Flow cytometric analysis revealed that compound 6 arrested cell cycle at G0/G1 phase and induced apoptotic cell death which was further confirmed by Hoechst staining, measurement of mitochondrial membrane potential (ΔΨm) and Annexin V-FITC assay. Thus, compound 6 can be considered as lead molecule for further development as potent anticancer therapeutic agent. This article is protected by copyright. All rights reserved. Menadione based triazole hybrids were synthesized by employing copper catalyzed azide-alkyne cycloaddition (CuAAC). The synthesized compounds were evaluated for their anticancer activity against five selected cancer cell lines. Compound 6 showed higher potency than the standard tamoxifen and parent menadione against MCF-7 cell line, arrested cell cycle at G0/G1 phase and induced apoptotic cell death.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.13073

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