Browsing by Author "Bildirici, I."

Now showing 1 - 2 of 2

Antiproliferative Effects of Pyranopyrazole Analogs: In Vitro and Molecular Docking Analysis
(KeAi Communications Co., 2026) Nalci, K.A.; Cetin, A.; Bildirici, I.; Bayram, U.F.
Background Glioblastoma multiforme is the most aggressive primary brain tumor in adults, and current multimodal therapies provide only limited survival benefit. There is an urgent need for new small-molecule scaffolds with improved anticancer activity against glioblastoma. Objective To evaluate the antiproliferative effects of pyranopyrazole analogs on human U-87 MG glioblastoma cells and to explore their potential molecular interactions with a glioblastoma-related protein target by molecular docking. Methods A series of pyranopyrazole analogs ( 12a – o ) was synthesized using a previously reported green-chemistry protocol. U-87 MG cells were treated with increasing concentrations of the analogs for 24, 48, and 72 h, and cell viability was measured by a colorimetric tetrazolium-based assay. Half-maximal inhibitory concentration values were determined for the most active analogs and compared with those of a reference chemotherapeutic agent. Molecular docking was performed with the 6c1c protein structure to assess binding energies and interaction profiles. Results Several pyranopyrazole analogs produced dose- and time-dependent cytotoxicity in U-87 MG cells. Analog 12 g showed the strongest antiproliferative effect and lower half-maximal inhibitory concentration values than the reference agent at earlier time points, whereas 12 h , 12o , and 12i displayed moderate activity. Docking analysis indicated favorable binding of active analogs to the 6c1c active site, with multiple hydrogen-bond and π-type interactions involving key residues. Conclusion Pyranopyrazole analogs, particularly 12 g , exhibit promising antiproliferative activity against glioblastoma cells in vitro, supported by compatible molecular docking findings. These compounds may represent useful lead structures for the development of new chemotherapeutic options for glioblastoma. © 2026 The Authors.
Trisubstituted Imidazole and N-Propargyl Imidazole Analogues: Synthesis, Characterization, in Silico Studies and Enzyme Inhibitory Properties
(Maik Nauka/interperiodica/springer, 2023) Altiok, M. S.; Cetin, A.; Kuzu, B.; Bildirici, I.
In recent years, the alpha-amylase, pancreatic lipase (PL), and beta-glucuronidase enzymes have received much attention as they promise to be potential drug targets for obesity and diabetes-related diseases. In this study, the synthesis and characterization of newly designed tricyclic imidazopyrrolopyrazine analogues with the potential to affect these enzymes were evaluated. The pharmacological evaluation of all imidazopyrrolopyrazine analogues revealed that all the synthesized analogues displayed excellent inhibitory effects against alpha-amylase, with the IC50 values of these analogues ranging from 4.05 +/- 0.7 to 5.61 +/- 0.8 mu M. The IC50 values of all synthesized analogues were also found to be effective inhibitors, ranging from 5.2 +/- 0.5 to 13.7 +/- 2.3 mu M, against pancreatic lipase. Furthermore, all analogues exhibited moderate inhibition in a wide range of 151.4 +/- 9.1 to 302.5 +/- 7.9 mu M against beta-glucuronidase. Additionally, all the synthesized analogues displayed moderate binding affinity with Ferric Reducing Antioxidant Power (FRAP), and low binding affinity with Oxygen Radical Absorbance Capacity (ORAC). This study provides valuable potential for the new tricyclic imidazopyrrolopyrazine analogues in further pharmacological studies.