Synthesis andin vitrobiological evaluation of new heterocycles based on the indole moiety

Abstract

New compounds based on the indole moiety were synthesized via the reaction of indole-3-carbinal 1 with different nucleophiles such as 6-aryl-[4-(2-methoxybenzyl)pyridazin-3-yl] hydrazones 2a-c, benzidine, 3,3 0 -dimethoxybenzidine 4a,b and 2,6-diaminopyridine 6 to afford hydrazine derivatives 3a-c and three different classes of bis-Schiff bases. The structures of the new compounds were elucidated on the basis of their FTIR, 1 H NMR, 13C NMR spectral data, GC/MS and elemental analysis. The antimicrobial activity of the new compounds was evaluated using a broth dilution technique in terms of minimal inhibitory concentration (MIC) against four pathogenic bacteria and two pathogenic fungi strains. Compound 14b showed excellent activity against Escherichia coli and Klebsiella pneumoniae. Some of the prepared compounds were tested for anti-cancer activity against human cell lines HCT116 (colon), MCF7 (breast) and HELA (cervix). From the results of the in vitro assays, compounds 3a,b, and 18a,c presented promising anti-cancer activity.

A novel bidentate ligand containing oxime, hydrazone and indole moieties and its BF2+ bridged transition metal complexes and their efficiency against prostate and breast cancer cells

“…If the results are compared with the familiar drug paclitaxel (1 μ m ), we can see that our products, especially Cu(II) and Co(II) complexes, can compete with this drug. New compounds like ours have been synthesized by Kandile et al [39] . who also used the indole moiety.…”

Antimicrobial activity of some pyrazolidin-3-one Schiff base derivatives and their complexes with selected metal ions

“…The minimum inhibitory concentration (MIC) was defined as the lowest concentration of experimental compounds that lead to a decrease in absorbance compared with that of the control (without experimental compounds). The MIC was determined in vitro in triplicate by broth dilution method [32] and average of them was considered. The reference drugs used were Ciprofloxacin as an antibacterial standard and fluconazole as an antifungal standard as shown in Figure 5.…”