Polat, Muhammed Fatih; İrem, Durmaz Şahi̇N; Atalay, Rengül; Tunçbi̇Lek, Meral

Cancer, a leading global cause of mortality, demands continuous advancements in therapeutic strategies. This study focuses on the design and synthesis of a novel series of purine derivatives, specifically 6-(substituted phenyl piperazine)-8-(4-phenoxyphenyl)-9-cyclopentyl purine derivatives (5–11). The motivation behind this endeavor lies in addressing acquired resistance mechanisms in cancer cells, a significant hurdle in current treatment modalities. The synthesis, starting from 4,6-dichloro-5-nitropyrimidine, involves a multi-step process, resulting in seven new purine derivatives. Biological evaluation against human liver, colon, and breast cancer cells (Huh7, HCT116, and MCF7, respectively) was performed using the SRB assay. Among the synthesized analogs, compounds 5 and 6, exhibited notable cytotoxic activity, surpassing clinically used positive controls 5-Fluorouracil and Fludarabine in terms of efficacy. This research underscores the potential of purine derivatives with a phenyl group at the C-8 position as a scaffold for developing compounds with improved anticancer properties. The findings offer insights for future exploration and development of novel agents in cancer pharmaceutical research.

Kahri̇Man, Nuran; Peker, Kıvanç; Serdaroğlu, Vildan; Aydin, Ali; Türkmenoğlu, Burçin; Usta, Asu; Yayli, Nurettin

In this study, syntheses of new pyrimidine-coupled N-β-glucosides and tetra-O-acetyl derivatives were carried out. All glycoconjugates were investigated in comparison with known chemotherapeutic agents in terms of their antimicrobial and anticancer functions and DNA/protein binding affinities. Spectral data showed that all glycoside derivatives were obtained by diastereoselectivity as β-anomers. Both tested groups exhibited strong antiproliferative activity (2.29–66.84 µg/mL), but some of them had sufficiently ideal % cytotoxicity values (10.01%–16.78%). And also all synthetic compounds exhibited remarkable antibacterial activity against human pathogenic bacteria. Binding of these compounds to CT-DNA resulted in significant changes in spectral properties, consistent with groove binding. Molecular docking studies of some compounds revealed that the docking score, complex energy, and MM-GBSA ΔGBind energy values were consistent with the experimental results, which showed that the new compounds were potent chemotherapeutic agents. Overall bioactivity results suggest that these compounds may be candidates as new chemotherapeutic agents and deserve further pharmacological evaluation.

Dursunoğlu, Benan; Yuca, Hafize; Gözcü, Sefa; Yilmaz, Bilal; Güvenalp, Zühal

Obesity is a serious disease that can be due to genetic and environmental reasons and is defined by the World Health Organization as abnormal or excessive fat accumulation that may impair health. There is an increasing trend towards herbal slimming products in obesity treatment. The quality control analysis of these products is important for public health. In this study, new, simple, and sensitive high performance liquid chromatography methods were developed for qualitative and quantitative determination of arbutin, hydroquinone, ursolic acid, chlorogenic acid, epigallocatechin gallate, epigallocatechin, epicatechin gallate, and catechin in eleven herbal slimming products in Turkey containing Camellia sinensis, Ilex paraguariensis, and Calluna vulgaris. The intra- and interday precisions, stated as the relative standard deviation, were less than 2% and accuracy, based on relative error, was less than 10%. The limits of detection and quantification for arbutin and hydroquinone were 0.80 and 2.40 µg/mL and for the other compounds were 0.30 and 0.90 µg/mL, respectively. The methods developed can be used for routine quality control analysis of these effective compounds in different herbal slimming products.

Çatir, Mustafa

Treatment of hydrogen peroxide with a polymer-supported hypervalent iodine compound, poly[4-diacetoxyiodo] styrene (PDAIS), generates singlet molecular oxygen (1O2). Singlet oxygen generation was proved by trapping with typical organic compounds such as conjugated dienes, aromatic dienes, and electron-rich alkene. When compared to monomer analogue, the use of PDAIS in peroxidation of substrates gave slightly better yields (45%–96%). Regeneration and reuse of PDAIS showed similar activity. The mechanism underlying generation of singlet oxygen and reaction scope was examined.