1. A new class of hybrid anticancer agents inspired by the synergistic effects of curcumin and genistein: Design, synthesis, and anti-proliferative evaluation.
- Author
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Chen, Qiao-Hong, Yu, Kevin, Zhang, Xiaojie, Chen, Guanglin, Hoover, Andrew, Leon, Francisco, Wang, Rubing, Subrahmanyam, Nithya, Addo Mekuria, Ermias, and Harinantenaina Rakotondraibe, Liva
- Subjects
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ANTINEOPLASTIC agents , *DRUG synergism , *GENISTEIN , *CURCUMIN , *DRUG design , *DRUG synthesis , *THERAPEUTICS - Abstract
Inspired by the synergistic effects of dietary natural products with different scaffolds on the inhibition of cancer cell proliferation, incorporation of central (1 E ,4 E )-1,4-penta-dien-3-one linker (an optimal substitute for the central metabolically unstable diketone linker of curcumin), 1-alkyl-1 H -imidazol-2-yl (a promising bioisostere of terminal aryl group in curcumin), and chromone (the common pharmacophore in genistein and quercetin) into one chemical entity resulted in ten new hybrid molecules, 3-((1 E ,4 E )-5-(1-alkyl-1 H -imidazol-2-yl)-3-oxopenta-1,4-dien-1-yl)-4 H -chromen-4-ones. They were synthesized through a three-step transformation using acid-catalyzed aldol condensation as key step. The WST-1 cell proliferation assay showed that they have greater anti-proliferative potency than curcumin, quercetin, and genistein on both androgen-dependent and androgen-independent human prostate cancer cells. [ABSTRACT FROM AUTHOR]
- Published
- 2015
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