Article
Chemistry, Medicinal
Jing Ma, Linrong Li, Kexin Yue, Zhansheng Zhang, Shihao Su, Yutong Chen, Lu Yu, Pengfei Zhang, Ruijuan Ma, Yingguang Li, Yinxia Ma, Huinan Jia, Chaojie Wang, Jiajia Wang, Songqiang Xie
Summary: A novel polyamine conjugate 13b demonstrated significantly elevated anti-tumor and anti-metastatic effects in vivo compared to a positive control, possibly through targeting multiple molecular mechanisms for inhibiting HCC metastasis, suggesting a promising strategy for treating HCC with reduced toxicities and notable activities.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Paula Costales, Nicolas Rios-Lombardia, Seila Lorenzo-Herrero, Francisco Moris, Javier Gonzalez-Sabin
Summary: A novel series of enantiopure naphthalimide-cycloalkanediamine conjugates were designed, synthesized and evaluated for their in vitro cytotoxicity. The cytotoxicity of the compounds depended on the size of the cycloalkyl ring and length of the spacer, with no observed enantioselectivity. Compounds 22 and 23 were found to effectively induce G2/M arrest in the tested cell lines, despite a mild apoptotic effect.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Matija Sambol, Patricia Bencic, Antonija Erben, Marija Matkovic, Branka Mihaljevic, Ivo Piantanida, Marijeta Kralj, Nikola Basaric
Summary: Quinone methide precursors with different alkyl linkers were synthesized and their photophysical properties, photochemical reactivity, and biological activities were investigated. Processes like photoinduced electron transfer and resonance energy transfer were found to play key roles in the fluorescence, complex formation, and anti-proliferative activity against cancer cells.
Article
Chemistry, Medicinal
Ming Zhang, Linming Li, Suying Li, Zhifang Liu, Ning Zhang, Bin Sun, Zhengping Wang, Dianlong Jia, Min Liu, Qingpeng Wang
Summary: A series of autophagy-targeted platinum(IV) conjugates incorporating an autophagy activator, clioquinol (CLQ), were designed. Among them, complex 5 with potent antitumor properties was selected as a candidate. Complex 5 showed significant antimetastatic properties both in vitro and in vivo by inducing DNA damage, promoting autophagy, and activating immunity. Key proteins associated with angiogenesis and metastasis, such as VEGFA, MMP-9, and CD34, were downregulated.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Anna Bogucka-Kocka, Przemyslaw Kolodziej, Anna Makuch-Kocka, Daria Rozycka, Sebastian Rykowski, Jan Nekvinda, Bohumir Gruner, Agnieszka B. Olejniczak
Summary: This study demonstrates the activity of a series of 1,8-naphthalimide-carborane/metallacarborane conjugates against Rhabditis sp. The conjugates with cobaltacarborane showed high activity compared to other carborane conjugates.
CHEMICAL COMMUNICATIONS
(2022)
Review
Biochemistry & Molecular Biology
Filippo Basagni, Giambattista Marotta, Michela Rosini, Anna Minarini
Summary: Over the past two decades, the strategy of conjugating polyamine tails with bioactive molecules has been widely used to enhance their pharmacological profile. Polyamine transport is increased in many pathological conditions, suggesting that the polyamine portion could improve cellular uptake of the conjugate. This review provides an overview of the polyamine conjugate scenario and highlights achievements and future developments.
Review
Chemistry, Multidisciplinary
Lihua Huang, Zonghao Sun, Qian Shen, Zhongxi Huang, Shuangxi Wang, Naidi Yang, Gongqiang Li, Qiong Wu, Wei Wang, Lin Li, Changmin Yu
Summary: This article provides an overview of the application of mitochondria-targeted nanocarriers in function regulation and discusses the advantages and disadvantages of different strategies for nanocarrier targeting of mitochondria. The article also explores the future prospects of mitochondria-targeted delivery systems in drug-based therapeutics.
CHINESE CHEMICAL LETTERS
(2022)
Article
Chemistry, Medicinal
Manoj Manickam, Pulla Reddy Boggu, Thanigaimalai Pillaiyar, Yeo Jin Nam, Md. Abdullah, Seung Jin Lee, Jong Seong Kang, Sang-Hun Jung
Summary: A series of potent naphthoquinone amines were synthesized and studied for their anticancer activity, in addition to the development of a tumor targeting drug delivery system using Biotin/polyamine conjugates.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Plant Sciences
Karina Vega-Granados, Marta Medina-O'Donnell, Francisco Rivas, Fernando J. Reyes-Zurita, Antonio Martinez, Luis Alvarez de Cienfuegos, Jose A. Lupianez, Andres Parra
Summary: A set of 12 maslinic acid-coumarin conjugates were synthesized, with one conjugate showing the most potent anticancer effects while maintaining high cell viability for non-tumor cells. Four conjugates demonstrated apoptotic effects in cancer cells, and most compounds caused cell-cycle arrest in the G0/G1 phase in all tested cancer cell lines.
JOURNAL OF NATURAL PRODUCTS
(2021)
Review
Chemistry, Multidisciplinary
Si Si Liew, Xiaofei Qin, Jia Zhou, Lin Li, Wei Huang, Shao Q. Yao
Summary: This review summarizes recent developments and strategies in the smart design of nanocarriers for mitochondria-targeted therapeutics, including subcellular targeting, stimuli-responsive nanocarriers, and synergistic therapy, while also discussing existing challenges and unexplored therapeutic opportunities.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Medicinal
Melissa M. Cadelis, Tim Liu, Kenneth Sue, Florent Rouvier, Marie-Lise Bourguet-Kondracki, Jean Michel Brunel, Brent R. Copp
Summary: Antibiotic resistance is a growing global health threat. One approach to overcome this is to discover and develop new antibiotic enhancers that can enhance the efficacy of existing antibiotics against resistant bacteria.
Article
Chemistry, Medicinal
Benjamin Rioux, Aline Pinon, Aurelie Gamond, Frederique Martin, Aurelie Laurent, Yves Champavier, Caroline Barette, Bertrand Liagre, Catherine Fagnere, Vincent Sol, Christelle Pouget
Summary: This study aimed to enhance bioavailability and selectivity of chalcone core towards cancer cells by synthesizing chalcone-polyamine conjugates, which showed significant anti-proliferative effects on colorectal and prostate cancer cell lines. The most active conjugate was found to inhibit cell proliferation by blocking the cell cycle at the G1 and G2 phase, and inducing apoptosis through several pro-apoptotic markers. The chalcone-N1-spermidine conjugate could be considered as a promising agent for colon and prostatic cancer adjuvant therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Jie Dong, Jie Qian, Kunqian Yu, Shuai Huang, Xiang Cheng, Fei Chen, Hualiang Jiang, Wenbin Zeng
Summary: Monitoring physiological changes of organelles is crucial for understanding cellular information and improving disease diagnosis and therapy. Fluorescent probes, considered as powerful imaging tools, have been widely used in biomedical fields. However, the design of these probes often lacks consistency with experimental results. To address this issue, we proposed a novel multi-level framework for predicting organelle-targeted fluorescent probes using advanced artificial intelligence algorithms. This approach not only provides a deeper understanding of the targeting mechanism but also enables quick evaluation and rational design. The optimized probes synthesized based on this methodology were verified for their targeting and imaging abilities through quantitative calculations and experiments.
Review
Pharmacology & Pharmacy
Varaporn Buraphacheep Junyaprasert, Parichart Thummarati
Summary: Polymer-drug conjugates (PDCs) have emerged as a versatile and effective approach to enhance cancer therapy. This review provides an overview of recent advancements in PDCs, including the choice of polymers, strategies for drug-polymer conjugation, and the importance of tumor-targeting ligands.
Article
Chemistry, Multidisciplinary
Yue Zhang, Anila Khalique, Xinchen Du, Zhanxia Gao, Jin Wu, Xiangyun Zhang, Ran Zhang, Zhiyuan Sun, Qiqi Liu, Zhelong Xu, Adam C. Midgley, Lianyong Wang, Xiyun Yan, Jie Zhuang, Deling Kong, Xinglu Huang
Summary: Integrating protein reconstruction technology and nanotechnology, an artificial hybrid nanozyme with superoxide dismutase and catalase-like activities was developed to target mitochondria and demonstrate protective effects in mitochondrial oxidative injury and heart function recovery. This innovative approach highlights the potential of enzyme mimics in regenerative medicine for alleviating oxidative damage.
ADVANCED MATERIALS
(2021)
Article
Oncology
Chaochao Ge, Yuxia Wang, Yongli Feng, Senzhen Wang, Kemeng Zhang, Xiaojuan Xu, Zhiyang Zhang, Yuan Zhao, Yanming Wang, Lei Gao, Fujun Dai, Songqiang Xie, Chaojie Wang
Summary: In this study, the novel naphthalimide derivative 6c was found to suppress CRC tumor growth and metastasis by inhibiting oxidative phosphorylation and the tricarboxylic acid cycle, leading to oxidative stress and inducing cell death and senescence. The combination of 6c and mitoxantrone showed stronger inhibitory effects on CRC by inducing reactive oxygen species production and autophagic cell death. These findings suggest that 6c may be a promising candidate for CRC treatment.
