In this study, carbazole (MC) and dibenzofuran (MD) derivatives were synthesized to examine their effect on the biomolecular recognition of G-quadruplex (G4) targets. Biophysical studies revealed that MC-4, a carbazole derivative, exhibits a specific affinity and effectively stabilizes the c-KIT 1 G4. Molecular modeling suggests a stable interaction of MC-4 with the terminal G-tetrad of c-KIT 1 G4. Biological studies demonstrate that MC-4 efficiently enters cells, reduces c-KIT gene expression, and induces cell cycle arrest, DNA damage, and apoptosis in cancer cells. These findings demonstrate MC-4 as a selective c-KIT G4 ligand with therapeutic potential, providing insight into the structural basis of its anticancer mechanisms.

中文翻译：

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通过杂芳族支架和侧链的结构调整选择性识别 c-KIT 1 G-四链体

在本研究中，合成了咔唑（ MC）和二苯并呋喃（MD ）衍生物，以检查它们对G-四链体（G4）靶标的生物分子识别的影响。生物物理学研究表明，咔唑衍生物MC-4具有特定的亲和力，可有效稳定c-KIT 1 G4。分子模型表明MC-4与c-KIT 1 G4的末端 G-四分体存在稳定的相互作用。生物学研究表明，MC-4可有效进入细胞，降低c-KIT基因表达，并诱导癌细胞周期停滞、DNA 损伤和细胞凋亡。这些发现证明MC-4作为一种具有治疗潜力的选择性c-KIT G4 配体，有助于深入了解其抗癌机制的结构基础。