By the reaction of substituted benzaldehydes and indol-3-carbaldehydes (2E)-2-cyano-N-[5-(R-benzyl)-1,3-thiazol-2-yl]-3-(R1-phenyl)prop-2-enamides 3-(1-R¹-1H-indol-3-yl)-2-cyano-N-(5-(R-benzyl)-1,3-thiazol-2-yl)prop-2-enamides were synthesised. The antitumor activity of prepared compounds were investigated. 3-(1-Benzyl-¹H-indol-3-yl)-2-cyano-N-(5-(2-chlorobenzyl)-1,3-thiazol-2-yl)prop-2-enamide (7b) has been identified as hit compound with values of MG-MID GI50 = 3.903 µM, TGI = 29.10 µM, LC50 = 57.54 µM.

A series of new derivatives of 3-(pyrrol-4-yl)acrylamides 3a-l with the pyrrole nucleus functionalized by chlorine atoms and ester group, have been synthesized by simple preparative methods from the available esters of 5-chloro-4-formylpyrrol-3-carboxylic acids 1a-e. At first, 3-(pyrrol-4-yl)acrylic acids 2a-e were synthesized by the Knoevenagel’s reaction between malonic acid and the esters 1a-e. Then the target compounds were obtained with a high yield in the reactions between chloroanhydrides of the synthesized acrylic acids and aromatic or aliphatic amines in the boiling benzene. The structure of all obtained compounds was confirmed by elemental analysis, IR, ¹H-NMR, and ¹³C-NMR spectroscopy, and additionally checked by the mass-spectrometry. Then the antimicrobial activity of all amides was tested in vitro on some gram-positive and gram-negative bacteria and fungi. It has been found that the gram-negative bacteria are resistant against the synthesized chemicals, while the gram-positive bacteria are sensitive to the amides 3с, e, f, g, i. The highest activity against Staphylococcus aureus MR and Staphylococcus epidermidis MS was registered for the amide 3f, and the retardation area diameter for this amide was greater than that for the control drugs.

In this study, seven cyano-benzylidene and bisbenzylidene derivatives were designed and synthesized. All synthesized compounds were evaluated to determine their insecticidal activities as potential insecticides against nymphs and adults of Aphis nerii. These efforts led to the discovery of compounds 3a-d, 5, 7 and 10 with potent insecticidal activity (LC50 range from 0.0141 to 3.4351ppm). Compound 5 exhibited the highest insecticidal potency with 0.0141ppm. In addition, it indicated that compound 3b is less toxic than benzylidene and other precursors. Therefore, our results suggest that compound 5 has strong potential as a candidate component for developing a novel eco-friendly insecticide for control Aphids.