Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives

Abstract

Seven novel derivatives of bis(2-aminoethyl)amine were synthesized. For compounds 1 and 7 single crystals were isolated and X-ray diffraction experiments were done. Lipophilicity and drug likeness were calculated in the initial stage of research. All compounds were screened for their in vitro cytotoxic activity against a panel of human cancer cell lines, which is contrary to normal (HaCaT) cell lines, by using the MTT method. Studies were followed by lactate dehydrogenase assay, apoptotic activity, and interleukin-6 assay. Within the studied group, compound 6 showed the most promising results in all biological studies. The strongest influence in A549 cells was denoted for derivative 4, which inhibited interleukin release almost tenfold, as compared to the control.

Synthetic Transition from Thiourea-Based Compounds to Tetrazole Derivatives: Structure and Biological Evaluation of Synthesized New N-(Furan-2-ylmethyl)-1H-tetrazol-5-amine Derivatives

“…The main goal in the current design was to replace the thiourea arrangement with a tetrazole scaffold. Twelve new N -(furan-2-ylmethyl)-1 H -tetrazol-5-amine derivatives were synthesized according to the well-known procedure [ 15 ]. Reaction conditions are depicted below ( Scheme 1 ).…”

“…A detailed description related to all conducted biological studies including cell culture, suitable conditions, and methodology was presented in our previous papers [ 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 37 ].…”

“…During previous years, our team also participated in research for new antimicrobial agents built on a tetrazole scaffold [ 13 , 14 , 15 ]. On the other hand, using our experience in working with other heterocyclic skeleton-based compounds [ 16 , 17 , 18 , 19 ] we have decided to design and synthesize a series of heterocyclic scaffold tetrazole hybrids [ 20 ].…”

Novel Tetrazole-Based Antimicrobial Agents Targeting Clinical Bacteria Strains: Exploring the Inhibition of Staphylococcus aureus DNA Topoisomerase IV and Gyrase

“…In previous years, our research group was devoted to searching for new tetrazole-based compounds with antimicrobial activity [ 22 , 23 , 24 , 25 ]. Clinicians use the tetrazole-derived antimicrobial drugs such as Cefamandole, Ceftezole, both second-generation broad-spectrum cephalosporin antibiotics, and the oxazolidinone-class antibiotic Tadalizolid.…”

“…Thiourea derivatives of two imides with confirmed antimicrobial activity were used as substrates for the synthesis of tetrazole-imide hybrids [ 29 , 30 ]. Our previous studies showed that the introduction of tetrazole arrangement in thiourea derivatives leads to an increase of antimicrobial activity [ 22 , 23 , 24 , 25 ].…”