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Synthesis and mechanistic studies of curcumin analog‐based oximes as potential anticancer agents
Author(s) -
Qin HuaLi,
Leng Jing,
Youssif Bahaa G. M.,
Amjad Muhammad Wahab,
Raja Maria Abdul Ghafoor,
Hussain Muhammad Ajaz,
Hussain Zahid,
Kazmi Syeda Naveed,
Bukhari Syed Nasir Abbas
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12964
Subject(s) - curcumin , chemistry , in vivo , cancer cell , kinase , cell culture , oxime , cancer , biochemistry , efflux , egfr inhibitors , pharmacology , biology , epidermal growth factor receptor , receptor , microbiology and biotechnology , genetics
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 BRAF V 600E 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 BRAF V 600E and EGFR ‐ TK kinases and also exhibited strong antiproliferative activity against different cell lines hence showing potential of multifunctional anticancer agents.

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