The synthesis of isoxazolino‐carbocyclic nornucleosides incorporating a quinoline moiety was tuned through nitrosocarbonyl intermediate chemistry, and a range of adenine analogues were attained through the linear construction of purine heterocyclic rings. The synthesis hinges on exo‐selective 1,3‐dipolar cycloaddition of quinolinenitrile oxide to the 2,3‐oxazanorborn‐5‐enes and simple elaboration of the cycloadducts. The nucleoside derivatives were initially tested for their inhibitory activity against a variety of viruses, including HBV, PTV and Flu A virus H1N1. High antiviral activities were found for compounds 22aA and 22bA in the case of Flu A H1N1.

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Influenza virus flu A H1N1 still remains a target for its inhibition with small molecules. Fleeting nitrosocarbonyl intermediates are at work in a short-cut synthesis of carbocyclic nucleoside analogues. The strategy of the synthetic approaches is presented along with the in vitro antiviral tests. The nucleoside derivatives were tested for their inhibitory activity against a variety of viruses. Promising antiviral activities were found for specific compounds in the case of flu A H1N1.

A new adenine derivative is prepared through the chemistry of nitrosocarbonyl intermediates. The synthesis relies upon the functionalization of adenine by inserting an ester moiety, to be transformed into the corresponding hydroxamic acid. The oxidation conducted in situ in the presence of cyclopentadiene afforded the hetero Diels‐Alder cycloadduct, furtherly elaborated to give the target nucleoside analogue. This single product displayed a selective high activity against HPV. The EC50 and EC90 values are remarkably lower than the values collected for Cidofovir used as control drug. The EC50 is 39 times lower while the CC50 value is 97.11 μM.

Background: Cancer is one of the greatest troubling maladies currently. It is believed that it is the second reason for death following cardiovascular maladies. Owing to the multiplicity of its types, stages and genetic basis, there is no existing drug to cure all types of cancer. Resistance to present drugs and severe adverse effects are other challenges in the struggle against cancer. In such pursuit, fluoroquinolones (FQs) have the potential as antiproliferative compounds due to safety, low cost, and absence of resistance. Aims: In this study, we aim to synthesize biologically active compounds that have dual anticancer and anti-lipase potential. Sixteen compounds were prepared, fully characterized, and studied through identification of IC50 values against the highly susceptible cancer cell lines. Methods: In this work we are concerned with synthesizing biologically active compounds that belong to fluoroquinolones (FQs) with dual anti-colorectal cancer and anti-lipase activity, owing to association between cancer and obesity, conduct titration and docking experiments to validate our hypothesis. Results: In vitro findings indicated that these compounds demonstrated promising anticancer activity against tested cell lines in micromolar range with a potency comparable to cisplatin. Compound 11 exhibited approximately doubled potency compared to cisplatin against SW620 colorectal cancer cell line with IC50 3.2 μM which proposes FQs as potent antiproliferative agents. The synthesized Fluoroquinolone (FQ) compounds were further screened for their in vitro anti-lipase potential. The findings demonstrated that all the screened compounds have demonstrated remarkable anti-lipase activity, as compared to control molecule orlistat. Compound 9 exhibited comparable activity to orlistat against pancreatic lipase with IC50 0.4 μM which proposes FQs as potent pancreatic lipase inhibitors. Conclusions: The anticancer potential of these derivatives is referred to their ability to inhibit Topo II which indicates that chelation is the mechanism of inhibition of Topo II emphasized with titration and docking experiments.