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

Synthesis and mechanistic studies of curcumin analog-based oximes as potential anticancer agents

Synthesis and mechanistic studies of curcumin analog-based oximes as potential anticancer agents
Syeda Naveed Kazmi, Jing Leng, Maria Abdul Ghafoor Raja, Bahaa G. M. Youssif, Syed Nasir Abbas Bukhari, Muhammad Wahab Amjad, Hua-Li Qin, Zahid Hussain, Muhammad Ajaz Hussain
The incidence of cancer can be decreased by chemoprevention using either natural or synthetic agents. Apart from synthetic compounds, numerous natural products have exhibited promising potential to inhibit carcinogenesis in vivo. In this study, α, β-unsaturated carbonyl-based anticancer compounds were used as starting materials to synthesize new oxime analogs. The findings from the antiproliferative assay using seven different human cancer cell lines provided a clear picture of structure–activity relationship. The oxime analogs namely 7a and 8a showed strong antiproliferative activity against the cell lines. The mechanistic effects of compounds on EGFR-TK kinases and tubulin polymerization and BRAFV600E were investigated. In addition, the efficacy of compounds in reversing the efflux-mediated resistance developed by cancer cells was also studied. The compounds 5a and 6a displayed potent activity on various targets such as BRAFV600E and EGFR-TK kinases and also exhibited strong antiproliferative activity against different cell lines hence showing potential of multifunctional anticancer agents. Newly synthesized oxime analogs showed strong antiproliferative activity against the cancer cell lines. The mechanistic effects of compounds on EGFR-TK kinases and tubulin polymerization and BRAFV600E were also investigated.

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

DOI: 10.1111/cbdd.12964

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