Some new 2-(2H-chromen-3-yl)-[1,3,4]oxadiazole derivatives 8a-e using Huisgen synthesis of 1,3,4-oxadiazoles reaction. Their structures were verified by 1H NMR and and elemental analyses. Compounds 8a-e were tested against 60 human cancer cell lines for in vitro cytotoxic activities according to the international scientific programme of the US National Institute of Health – DTP (Developmental Therapeutics Program), National Cancer Institute (Bethesda, Maryland, USA). Compounds with moderate activity against certain cancer cell lines were identified. In addition, in collaboration with CO-ADD (The Community for Open Antimicrobial Drug Discovery), we have studied the antibacterial activity against the ESCAPE group of strains and the antifungal activity against C. Albicans ATCC 90028 and C. Neoformans ATCC 208821. The studies allowed us to identify 3-[5-(6-bromo-2H-chromen-3-yl)-[1,3,4]oxadiazol-2-yl]-pyridine as a compound with high antibacterial activity against E. Coli ATCC 25922 with MIC 8 μg/ml. Docking studies have shown high affinity of this compound for the bacterial DNA gyrase of Escherichia coli.

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.

Novel 2,4-disulfonylsubstituted 5-aminothiazoles were synthesized and their anticancer activity was assessed at a high dose (10 μM) against NCI 60 cancer cell lines. Compounds 24 and 25 showed the antiproliferative activity with mean growth inhibition about 66.0%. Replacing 4-hydroxypiperidine 24 with the more hydrophilic N-methyl piperazine 25 increased the number of sensitive cell lines while replacing these hydrophilic groups with lipophilic ones abolished the anticancer activity. The COMPARE analysis showed that the tested compounds had a moderate positive correlation with alkylating agents (CCNU and methyl CCNU) and with a purine nucleotide biosynthesis inhibitor analog (L-cysteine). The results indicate that the above mechanisms of antitumor action of standard compounds are not the main ones for the tested compounds due to the lack of a high correlation. The results of this study allow us to consider compounds 24 and 25 as a basis for their further functionalization to obtain more active compounds.

A famous cisplatin anticancer agent is one of the most widely used chemotherapeutics for treating several human solid tumors. Toxicity of the normal cell is a life-threatening issue that restricts the therapeutic potential of cisplatin complex as an anticancer drug. Even though every year thousands of cisplatin-based analogs have been prepared, screened, and reported, only very few compounds entered the medical trials. Hence, new research work is still sensible. In the last few years, many mononuclear and polynuclear platinum complexes have been considerably investigated, in vitro and in vivo studies evaluated, with some compounds demonstrating significant anticancer potential. In this review, various mono-metallic and poly-metallic platinum‐based complexes with various derivatives used as ligands that have anticancer potential are defined and numerous typical examples are discussed briefly. Present investigation, numerous mononuclear cisplatin derivatives exhibited greater anticancer potency than the parent cisplatin drug. However, polynuclear cisplatin derivatives showed much better anticancer activity than mononuclear cisplatin analogs against various cancer cell lines.

In the present work, we presented an efficient synthesis and anticancer activity evaluation of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. We have shown that the proposed synthetic protocols provided the possibility to design triazolothiadiazoles diversity with a considerable chemical novelty. The structures of target substances were confirmed by using 1H NMR spectroscopy, mass spectrometry and elemental analysis. The synthesized compounds were selected by the National Cancer Institute Developmental Therapeutic Program for the in vitro cell line screening. Among all the substances tested, three compounds exhibited significant cytotoxic activity.

Spodopetra Frugiperda is a highly polyphagous migratory lepidopteran pest species. It causes infestation in crops leading to severe crop losses. Being a new invasive parasite, its susceptibility to insecticides needs to be explored and therefore, there is an urgent need to develop the potent insecticides for the effective control of this insect pest. This is the first report on toxic effects produced by the prepared chalcone and hydrazone analogs, followed by structure relationships. Five compounds of chalcone and hydrazone derivatives have been synthesized in pure state as reported procedures, and their toxicity as potential insecticidal agent against Spodopetra Frugiperda was screened. Their characterizations by using spectroscopic analyses were performed. The toxicity data exhibited that compound 5 is more toxic about 2-fold than other synthesized compounds, the other screened compounds showed weak to strong toxicological activity against Spodopetra Frugiperda (lepidoptera: Noctuidae).

The synthesis, anticancer and antimicrobial properties of novel N-aryl-2-(5-aryltetrazol-2-yl)acetamides were discussed. Novel N-aryl-2H-tetrazoles were synthesized and modified in order to obtain the compounds with a satisfactory pharmacological profile. The structures of target substances were confirmed by using ¹H spectroscopy, mass spectrometry and elemental analysis. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). The compounds with significant levels of anticancer activities have been found that can be used for further optimization. The antimicrobial activity of the synthesized substances was evaluated by the value of the MIC and minimum fungicidal and bactericidal concentration. The findings exhibited that the compounds possessed moderate antimicrobial potential.

Two heterocyclic Schiff bases namely (E)-2-(1-(2-phenylhydrazono)ethyl)pyridine (or 2-acetyl pyridine phenyl hydrazone) (2APPH) and (E)-2-(1-triazylidineethyl)pyridine (or 2-acetyl pyridine semicarbazone) (2APSC) were synthesized, characterized and their corrosion inhibition behaviour as well as mechanism of inhibition were investigated by different techniques. Structural characterization includes NMR, Mass, IR and UV-visible spectroscopy and elemental analysis. Corrosion inhibition behaviour of aforesaid compounds on mild steel in 1M hydrochloric acid was examined by electrochemical methods including potentiodynamic polarization analysis and electrochemical impedance spectroscopic techniques. The mechanism of corrosion inhibition was explored and supplemented by adsorption and surface morphological studies. Quantum mechanical investigations on corrosion behaviour of compounds were also conducted and satisfying correlation was noticed between the results of corrosion measurement methods and quantum mechanical evaluations.

Obtained by the interaction of 2-amino-3,3-dichloroacrylonitrile and chlorosulphonyl isocyanate (Z)-(5-(dichloromethylene)-2-oxoimidazolidin-4-ylidene)sulfamoyl chloride reacts easily with excess of the aliphatic amine to form new (Z)-N-(5-(dichloromethylene)-2-oxoimidazolidin-4-ylidene)-N'-substituted sulfonamides. According to the National Cancer Institute (USA) examinations, two of the six synthesized sulfonamides showed a high anticancer activity.