Design, Synthesis and Cytotoxicity of New Coumarin-1,2,3-triazole Derivatives: Evaluation of Anticancer Activity and Molecular Docking Studies.

A library of new coumarin-1,2,3-triazole hybrids 7a-l were synthesized from 4-(diethylamino)-2-hydroxybenzaldehyde precursor through a series of reactions including Vilsmeier-Haack reaction and condensation reaction to achieve key intermediate oxime and further performed click reaction by using different aromatic azides. We screened all molecules in silico against crystal structure of Serine/threonine-protein kinase 24 (MST3), based on these results all molecules were screened for their cytotoxicity against human breast cancer MCF-7 and lung cancer A-549 cell lines. Compound 7 b (p-bromo) showed best activity against both cell lines MCF-7 and A-549 with IC value of 29.

Palladium(ii)-catalyzed synthesis of indenones through the cyclization of benzenecarbaldehydes with internal alkynes.

The palladium(ii)-catalyzed carbocyclization of benzenecarbaldehydes with internal alkynes to afford 2,3-disubstituted indenones was reported. The annulation reaction proceeded through the transmetalation of Pd(ii) with an aromatic aldehyde and the insertion of internal alkynes, followed by cyclization the intramolecular nucleophilic addition of intermediate organopalladium(ii) species to the aldehyde group. This reaction proceeded in moderate to good yields with high regioselectivity.

2,3-Dihydrofurans as Potential Cytotoxic and Antibacterial Agents: Tandem Knoevenagel-Michael Cyclization for the Synthesis of 2,3-Dihydrofurans by Using α-Tosyloxy Ketone Precursors.

Novel 2,3-dihydrofuran derivatives were synthesized through a tandem Knoevenagel-Michael cyclization in good yield by reacting α-tosyloxy ketone, 5,5-dimethyl-1,3-cyclohexanedione, and various aldehydes in the presence of phthalazine in acetonitrile. These compounds were subjected to in vitro antibacterial screening against eight micro-organisms by using diffusion method and also in vitro cytotoxicity screening against four human cancerous cell lines by applying MTT assay. Some of the compounds showed impressive activities.

Stereoselective total synthesis of a novel regiomer of herbarumin I and its cytotoxic and antimicrobial activities.

Stereoselective synthesis of a novel regiomer of the natural nonenolide, herbarumin I has been accomplished. The synthesis involves the coupling of the alcohol and acid fragments of the molecule using Yamaguchi protocol followed by intramolecular ring closing metathesis. The cytotoxic and antimicrobial properties of the synthetic regiomer have been studied.