We report here the synthesis of a novel branched quasi-dendric system, 9,9′-(9,9′-dihexylfluorene-2,7-diyl)bis[3,6-bis(2,5-bis(2-thienyl)pyrrol-1-yl)carbazole], (FCSNS), in four steps, followed by coating onto an ITO-coated glass surface by an electropolymerization process to give a very stable cross-linked polymeric film (poly-FCSNS). The yellowish-green color of this film in its neutral state changed reversibly to black upon oxidation. An electrochromic device, assembled in the sandwich configuration [ITO/anodically coloring polymer (poly-FCSNS)//gel electrolyte//cathodically coloring polymer/(PEDOT)/ITO], exhibited a relatively short response time (about 1 s), a high redox stability, and a high coloration efficiency (1624 cm²C⁻¹). In addition to electrochromic studies, organic light-emitting diode (OLED) work was also carried out using FCSNS. A multilayer OLED having a configuration of ITO/PEDOT:PSS/FCSNS/Alq₃/LiF : Al was fabricated, and it showed a turn-on voltage of approximately 6 V and exhibited a bright green emission with a luminance of 3700 cd m⁻². The maximum luminous efficiency was found to be 2.0 cd A⁻¹ at 14 V and 11.75 mA cm⁻². The emitted light from the OLED device is green, and has the color coordinates of (x, y) (0.33, 0.54) according to CIE. Electrochemical and optical properties were also studied by using cyclic voltammetry, UV-Vis absorption and fluorescence spectroscopy, respectively.

Imatinib, an Abelson (ABL) tyrosine kinase inhibitor, is a lead molecular-targeted drug against chronic myelogenous leukemia (CML). To overcome its resistance and adverse effects, new inhibitors of ABL kinase are needed. Our previous study showed that the benzyl ester of gypsogenin (1c), a pentacyclic triterpene, has anti-ABL kinase and a subsequent anti-CML activity. To optimize its activities, benzyl esters of carefully selected triterpenes (PT1–PT6), from different classes comprising oleanane, ursane and lupane, and new substituted benzyl esters of gypsogenin (GP1–GP5) were synthesized. All of the synthesized compounds were purified and charachterized by different spectroscopic methods. Cytotoxicity of the parent triterpenes and the synthesized compounds against CML cell line K562 was examined; revealing three promising compounds PT5, GP2 and GP5 (IC₅₀ 5.46, 4.78 and 3.19 μM, respectively). These compounds were shown to inhibit extracellular signal-regulated kinase (ERK) downstream signaling, and induce apoptosis in K562 cells. Among them, PT5 was identified to have in vitro activity (IC₅₀ = 1.44 μM) against ABL1 kinase, about sixfold of 1c, which was justified by molecular docking. The in vitro activities of GP2 and GP5 are less than PT5, hence they were supposed to possess other more mechanisms of cytotoxicity. In general, our design and derivatizations resulted in enhancing the activity against ABL1 kinase and CML cells.

4-[(3-Methylphenyl)(phenyl)amino]benzoic acid (MPPBA) was synthesized in order to facilitate the hole-injection in Organic Light Emitting Diodes (OLED). MPPBA was applied to form self-assembled monolayer (SAM) on indium tin oxide (ITO) anode to align energy-level at the interface between organic semiconductor material (TPD) and inorganic anode (ITO) in OLED devices. The modified surface was characterized by X-ray photoelectron spectroscopy (XPS), atomic force microscopy (AFM) and Kelvin probe force microscopy (KPFM). KPFM was used to measure the surface potential and work function between the tip and the ITO surface modified by SAM technique using MPPBA. The OLED devices (ITO/MPPBA/TPD/Alq3/Al) fabricated with SAM-modified ITO substrates showed lower turn-on voltages and enhanced diode current compare to the OLED devices fabricated with bare ITO substrates.TUBITAK Grant No. TBAG-108T71

Glioma, particularly its most malignant form, glioblastoma multiforme (GBM), is the most common and aggressive malignant central nervous system tumor. The drawbacks of the current chemotherapy for GBM have aroused curiosity in the search for targeted therapies. Aberrantly overexpressed epidermal growth factor receptor (EGFR) in GBM results in poor prognosis, low survival rates, poor responses to therapy and recurrence, and therefore EGFR-targeted therapy stands out as a promising approach for the treatment of gliomas. In this context, a series of pentacyclic triterpene analogues were subjected to in vitro and in silico assays, which were conducted to assess their potency as EGFR-targeted anti-glioma agents. In particular, compound 10 was the most potent anti-glioma agent with an IC₅₀ value of 5.82 µM towards U251 human glioblastoma cells. Taking into account its low cytotoxicity to peripheral blood mononuclear cells (PBMCs), compound 10 exerts selective antitumor action towards Jurkat human leukemic T-cells. This compound also induced apoptosis and inhibited EGFR with an IC₅₀ value of 9.43 µM compared to erlotinib (IC₅₀ = 0.06 µM). Based on in vitro and in silico data, compound 10 stands out as a potential orally bioavailable EGFR-targeted anti-glioma agent endowed with the ability to cross the blood–brain barrier (BBB).

Background: Despite recent breakthroughs in cancer treatment, non-small cell lung cancer (NSCLC) and breast cancer remain major causes of death from all malignancies. The epidermal growth factor receptor (EGFR) is an important mediator of the pathways involved in cell proliferation, apoptosis, and angiogenesis. Thus, its overexpression triggers several types of cancer, including NSCLC and breast cancer. Methods: In the current study, we synthesized new pyrimidine-tethered compounds (chalcone derivative (B-4), pyrazoline–carbothioamide (B-9), and pyrazoline–thiazole hybrids (BH1-7)). These compounds were then tested for cytotoxicity against A549 NSCLC and MCF-7 breast cancer cells. Results: Of these, B-4 displayed significant cytotoxicity against both cells (IC₅₀ = 6.70 ± 1.02 µM for MCF-7; IC₅₀ = 20.49 ± 2.7 µM for A549) compared to the standard agent lapatinib (IC₅₀ = 9.71 ± 1.12 µM for MCF-7; IC₅₀ = 18.21 ± 3.25 µM for A549). The anticancer potential of B-4 between Jurkat leukemic T cells and peripheral blood mononuclear cells (PBMCs) (healthy) was found to be selective. Mechanistically, 11.9% and 10.2% of A549 and MCF-7 cells treated with B-4, respectively, underwent apoptosis and B-4 produced 46% EGFR inhibition at a concentration of 10 μM. The B-4/EGFR complex obtained after induced fit docking was subjected to 300 ns of molecular dynamics simulation, which confirmed the stability of the complex in a mimicked biological environment. On the other hand, B-4 was shown to have drug-like properties by in silico pharmacokinetic estimation. Conclusions: B-4 is an EGFR inhibitor and apoptosis inducer for future NSCLC and breast cancer studies.