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A novel series of chalcones and flavanones discriminated by the presence of a 3,4-dimethoxyphenyl moiety in their structures were synthesized as anti-cancer agents. The cytotoxicity evaluation of the analogs against the MCF-7, MDA-MB-231 (human breast cancer), and SK-N-MC (human neuroblastoma) cell lines demonstrated that the introduction of a halogen on the 3,4-dimethoxyphenyl part of both series and the attachment of a pyrrolidinylethoxy group on the C-7 position of the flavanone derivatives increased their activity. Indeed, 3-halogenated chalcones (1c and 1d) were more potent than the standard drug etoposide against all tested cell lines. Fluorescence microscopy and flow cytometry analyses confirmed that the anti-cancer effect of the most potent compounds 1c and 1d occurs via apoptosis induction.

A new metal‐free decarboxylative coupling reaction between coumarin‐3‐carboxylic acid derivatives, formaldehyde, and amines is developed. The use of water as the solvent without using any catalyst or additive, excellent functional group tolerance, and good yields are the beneficial features of this synthetic pathway. The cholinesterase inhibitory activity of some selected target compounds is also evaluated.

A novel series of 2‐acetamide‐5‐phenylthio‐1,3,4‐thiadiazol derivatives containing a phenyl urea warhead were synthesized and evaluated as antiproliferative agents. The cytotoxic activities of the newly synthesized compounds were evaluated toward three human cancer cell lines, including HT‐29, A431, and PC3, as well as normal HDF cells, using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyl tetrazolium bromide assay. The biological results revealed the highest degree of cytotoxic effects for the 4‐chloro‐containing compound 9e against the A431 cell line. Further assessment by Western blot analysis assay confirmed the induction of apoptosis by compound 9e, with upregulation of Bax and downregulation of Bcl‐2 proteins in A431 cancer cells. In addition, compound 9e inhibited the phosphorylation of vascular endothelial growth factor and its receptor (VEGFR‐2) in A431 cancer cells while the total level of actin protein was unchanged. These results were confirmed by a three‐dimensional cell culture method using the hanging drop technique.

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