From Natural Limonoids to a Rationally Designed Derivative: Facilitating the Study of Anti-Adenocarcinoma Potential and Mechanisms Through Solubility Enhancement [0.03%]
从天然柠檬苦素到理性设计衍生物:通过提高溶解性促进抗腺癌潜力和机制研究
Juan Guo,Xinyi Luo,Zexin Chen et al.
Juan Guo et al.
Natural limonoids, exemplified by limonin from lemon seeds, exhibit promising antitumor activity but are hindered by poor aqueous solubility, which critically limits their bioavailability and cellular engagement. To address this, a rational...
Selective Estrogen Receptor Modulators (SERMs): Advances, Challenges, and Future Prospects in ER+ Breast Cancer Therapy [0.03%]
选择性雌激素受体调节剂(SERM)在ER阳性乳腺癌治疗中的进展、挑战和未来前景
Anurag Saini,Ripunjay Kalita,Tirtha Nath et al.
Anurag Saini et al.
Selective estrogen receptor modulators (SERMs) are an important class of drugs mainly useful in the treatment of breast cancer as they act as estrogen antagonists in the breast tissue but have an agonistic activity in bone and the cardiovas...
Advances in Platinum(IV) Functional Axial Ligand Research: A Prospective Perspective [0.03%]
铂(IV)功能轴向配体研究进展:展望视角
Zhenjie Cheng,Mei Zhu,Tianyu Wu et al.
Zhenjie Cheng et al.
Malignant tumors have become the second leading cause of death after cardiovascular and cerebrovascular diseases, with their incidence and mortality rates remaining persistently high. Since the discovery of cisplatin's potent antitumor effe...
Discovery of Novel HPK1 Inhibitors via High-Throughput Virtual Screening, Biological Evaluation, and Molecular Dynamics Simulation [0.03%]
基于高通量虚拟筛选、生物活性评价和分子动力学模拟的HPK1抑制剂的研究发现
Xinglong Chi,Yiqun Chu,Roufen Chen et al.
Xinglong Chi et al.
Hematopoietic progenitor kinase 1 (HPK1) acts as a negative regulator of T-cell receptor signaling, making it a high-priority target for cancer immunotherapy. Addressing the scarcity of structurally novel HPK1 inhibitors, we constructed and...
Advances in Five-Membered Heterocyclic Scaffolds as Anti-Tuberculosis Agents: A Decade of Discovery [0.03%]
作为抗结核药物的五元杂环支架的研究进展:十年成果回顾
P Tejaswani,Debashis Das,Spandan Kumar et al.
P Tejaswani et al.
Tuberculosis remains a deadly infectious disease with 1.09 million deaths and 10.8 million new cases reported in 2023. Escalating drug resistance and mortality rates worsen the situation. To address these issues, new TB agents with improved...
Harmine Derivatives as Anticancer Agents Endowed With Potent and Selective Antileukemia Activity: Synthesis, Biological Evaluation, Proapoptotic and Genotoxic Activity [0.03%]
赋予抗白血病活性的抗肿瘤药羟亚胺衍生物:合成、生物学评价以及致凋亡和致基因毒活性
Abdul Aziz Timbilla,Filip Pidany,Eliska Kohelova et al.
Abdul Aziz Timbilla et al.
β-Carboline alkaloids, such as harmine (1), have demonstrated notable anticancer properties, making them attractive candidates for anticancer drug development. This study evaluated the antiproliferative activity of compound 1 and thirty-th...
Berberine C9-Derivatives Selective Cytotoxicity Depends on Balance Between Mitochondrial Damage and DNA Intercalation [0.03%]
小分子选择性杀伤肿瘤的平衡模型:线粒体靶向与DNA插入共同决定伯克敏类化合物的选择性 cytotoxicity
Anastasiia Yu Kolchanova,Konstantin G Lyamzaev,Nicolae Valutsa et al.
Anastasiia Yu Kolchanova et al.
Berberine, a naturally occurring compound, inhibits the growth of cancer cells in vitro at micromolar concentrations. Selective cytotoxicity was revealed for berberine derivatives and monoterpene aminoalcohols in the FCCT (fluorescent cells...
Harnessing Hybrid Chemistry: Novel Ethyl Ferulate Ester of Niflumic Acid for Enhanced Therapeutic Benefits [0.03%]
利用杂化化学:尼氟灭酸乙基 ferulate 酯用于增强治疗效益的新方法
Rahila P Chavilkad,Ramsiya Kottassery,Shafnaz A Rahman et al.
Rahila P Chavilkad et al.
Niflumic acid is a potent NSAID, while its long-term therapy can cause gastrointestinal complications. This study explores the prodrug approach of niflumic acid with natural antioxidant ethyl ferulate to improve its pharmacokinetics, thereb...
Enabling Green Analytical Chemistry: An Automated Chemometric Framework for Spectrophotometric Quantification of Veterinary Drugs [0.03%]
开启绿色分析化学:兽药分光光度法定量的自动化 chemometrics 框架
Ayman M Algohary,Sultanah M N Alhunayhin,Belal Muneeb Kanaan et al.
Ayman M Algohary et al.
Effective pain management in veterinary medicine often utilizes multi-drug formulations containing Metamizole sodium (MT), Paracetamol (PA), and Diclofenac (DI). However, severe spectral overlap makes their simultaneous quantification by sp...
Decoding MYC Targeted Inhibition in Cancer: Integrating Medicinal Insights With Computational Design Approaches [0.03%]
基于药物研发的MYC癌基因抑制计算设计方法学体系研究综述
Subhankar Pradhan,Shivani Kasana,Balak Das Kurmi et al.
Subhankar Pradhan et al.
The MYC family of oncoproteins, a central regulator of cellular proliferation and metabolism, is aberrantly regulated in over 70% of human cancers, making them a significant target for therapeutic intervention. Yet, MYC intrinsically disord...