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Biochemistry & Molecular Biology
Olga Michalak, Marcin Cybulski, Wojciech Szymanowski, Agnieszka Gornowicz, Marek Kubiszewski, Kinga Ostrowska, Piotr Krzeczynski, Krzysztof Bielawski, Bartosz Trzaskowski, Anna Bielawska
Summary: A series of new derivatives of ursolic acid (UA) were designed and synthesized by substituting various amino acids (AAs) or dipeptides (DP) at the C-3 position of the steroid skeleton. These conjugates exhibited cytotoxic activity against hormone-dependent and triple-negative breast cancer cells. Mechanistic studies revealed the activation of apoptotic pathways for some compounds and the induction of autophagy for others. Additionally, the synthesized compounds showed potential as anticancer agents based on their ADME properties and molecular docking to the estrogen receptor.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Ju Chen, Yunran Xu, Yan Yang, Xin Yao, Yuan Fu, Yi Wang, Yunjun Liu, Xiuzhen Wang
Summary: In this study, a series of glycyrrhetic acid derivatives were synthesized and their cytotoxicity against tumor cells was investigated. Compound 3a showed high antiproliferative activity against HeLa cells and its mechanism of action was explored through various assays. The results demonstrated that compound 3a could block the cell cycle, inhibit cell migration, induce apoptosis, and affect the expression of mitochondria-related proteins. This work provides valuable insights for the development of glycyrrhetinic acid compounds as potential anticancer molecules.
Article
Chemistry, Medicinal
Linling Gan, Zongjie Gan, Yanrong Dan, Yaowei Li, Peiming Zhang, Shanwen Chen, Zaijun Ye, Tao Pan, Chunmei Wan, Xuelian Hu, Yu Yu
Summary: A series of novel TNBG analogues were developed, among which compound 14g exhibited strong inhibitory effects on HepG2 and A549 cells, possibly through the activation of PPARγ expression. In an in vivo xenograft model, 14g effectively reduced tumor growth and demonstrated excellent water solubility.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Lin Wang, Maoling Yao, Yuegao Hu, Congdi Chen, Liming Jin, Xiaodong Ma, Hongjun Yang
Summary: In this study, two series of diosgenin derivatives were synthesized and evaluated for their cellular anticancer activities. The representative compound 2.2f exhibited significantly higher antiproliferative activities against four cell lines compared with the lead compound diosgenin.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Pharmacology & Pharmacy
Xi-Xi Hou, Long-Fei Mao, Yajie Guo, Chaoxuan Lou, Lan Wang, Rui-Fang Li, Huili Wang, San-Qiang Li, Jian-Xue Yang
Summary: Based on structural modification, novel dolutegravir derivatives containing 1,2,3-triazole moieties with different substituted groups were synthesized. The derivatives exhibited good inhibitory effects on A549 cells, with compounds 4b and 4g being the most effective, showing IC50 values of 8.72 +/- 0.11 mu M and 12.97 +/- 0.32 mu M, respectively. Furthermore, compound 4g induced apoptosis and clonal suppression in A549 tumor cells, activated LC3 signaling pathway to induce autophagy, and activated gamma-H2AX signaling pathway to induce DNA damage in tumor cells.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Fernando Duraes, Patricia M. A. Silva, Pedro Novais, Isabel Amorim, Luis Gales, Catia I. C. Esteves, Samuel Guieu, Hassan Bousbaa, Madalena Pinto, Emilia Sousa
Summary: A library of thioxanthones was synthesized, leading to unexpected discovery of four tetracyclic thioxanthenes. Two compounds exhibited potent growth inhibition in human tumor cell lines, with established structure-activity relationship. Photophysical studies revealed dye-like characteristics in some compounds.
Review
Biochemistry & Molecular Biology
Qiuzi Dai, Qinsheng Sun, Xiaorong Ouyang, Jinyang Liu, Liye Jin, Ahao Liu, Binsheng He, Tingting Fan, Yuyang Jiang
Summary: 1,3,5-triazine derivatives, also known as s-triazines, have shown their potential as anticancer agents. Several s-triazine derivatives have been approved for the treatment of refractory ovarian cancer, metastatic breast cancer, and leukemia. This review focuses on the medicinal chemistry of s-triazines and their targeting of topoisomerases, tyrosine kinases, phosphoinositide 3-kinases, NADP+-dependent isocitrate dehydrogenases, and cyclin-dependent kinases in various signaling pathways. It provides a comprehensive summary of the discovery, structure optimization, and biological applications of these s-triazine derivatives as anticancer drugs.
Article
Chemistry, Medicinal
Liwei Ma, Jinling Zhang, Xuemei Wang, Jifang Yang, Lina Guo, Xiaoli Wang, Bo Song, Wei Dong, Wenbao Wang
Summary: DSG-amino acid ester derivatives showed cytotoxic activities against various human cancer cell lines, with compound 7g exhibiting the most significant cytotoxicity against the K562 cell line. Mechanistic studies revealed that compound 7g induced mitochondrial-related apoptosis in K562 cells, highlighting its potential as a promising scaffold for the development of more potent anticancer agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Anita Bulakowska, Jaroslaw Slawinski, Rafal Halasa, Anna Hering, Magdalena Gucwa, J. Renata Ochocka, Justyna Stefanowicz-Hajduk
Summary: In this study, ten new N-(4-chloro-2-mercapto-5-methylphenylsulfonyl)cinnamamide derivatives were synthesized. These compounds showed antimicrobial activity against Staphylococcus and Enterococcus species, inhibited biofilm formation, and exhibited cytotoxic activity on cancer cells. The results suggest that these synthesized derivatives have potential as antimicrobial therapeutic agents.
Article
Biochemistry & Molecular Biology
Judson Vincent Edwards, Nicolette T. Prevost, Dorne Yager, Robert Mackin, Michael Santiago, SeChin Chang, Brian Condon, Joseph Dacorta
Summary: The development of affordable and environmentally friendly barrier fabrics with antimicrobial properties is a current focus in textile research. This study demonstrates the antimicrobial and antiviral properties of spunlaced griege cotton nonwovens treated with ascorbic acid formulations. By promoting enhanced hydrogen peroxide activity, these fabrics show efficacy against both Gram-negative and Gram-positive bacteria, as well as MS2 bacteriophages. A low-cost method for covalent attachment of ascorbic acid to cellulose is also discussed. These findings suggest a simple approach to producing antimicrobial and antiviral cotton-based nonwovens for various applications.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Louise Idalgo Vasques, Cristina Wohlke Vendruscolo, Gislaine Ricci Leonardi
Summary: The topical application of vitamin C and its derivatives in skincare is essential, but there is still a lack of scientific data regarding their efficacy, especially in vivo. Studies on the stability, safety, adverse reactions, and efficacy with standardized parameters and a relevant number of subjects are necessary for better understanding their effects.
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Physical
Dobrawa Kwasniewska, Justyna Kiewlicz
Summary: The interactions between the cationic surfactant CTAB and ascorbic acid and its derivatives in aqueous media were investigated. Surface tension isotherms were used to determine the critical micelle concentration and adsorption parameters. Infrared analysis contributed to estimating the existence of interactions in the systems. The effect of CTAB-ascorbic acid/ascorbic acid derivatives interactions on antioxidant activity was analyzed.
JOURNAL OF MOLECULAR LIQUIDS
(2022)
Article
Biochemistry & Molecular Biology
Huixin Liang, Wei Wang, Fugui Zhu, Shuqiang Chen, Dan Liu, Chunquan Sheng
Summary: A series of novel bis-evodiamine derivatives inspired by the antitumor natural product evodiamine were synthesized, and they exhibited potent antitumor activity. Notably, compound 13b effectively inhibited the proliferation and migration of HCT116 cells. Mechanistic studies further revealed that compound 13b induced apoptosis in HCT116 cells and arrested the cell cycle at the G2/M phase. Therefore, compound 13b represents a promising lead compound for the discovery of novel antitumor agents.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Han Luo, Yong-Feng Lv, Hong Zhang, Jiang-Miao Hu, Hong-Mei Li, Shou-Jin Liu
Summary: A new series of mollugin-1,2,3-triazole derivatives were synthesized using a copper(I)-catalyzed Huisgen 1,3-dipolar cycloaddition reaction, and most of them demonstrated cytotoxicity on five human cancer cell lines, with compounds 14 and 17 showing significant cytotoxicity across all five cancer cell lines.
Article
Biochemistry & Molecular Biology
Hong-Wei Jia, Hua-Li Yang, Zhi-Ling Xiong, Ming-Hui Deng, Tong Wang, Yang Liu, Maosheng Cheng
Summary: In this study, 38 acrylamide derivatives were designed and synthesized, and these compounds exhibited effective IMPDH inhibitory activity and played a significant role in cancer intervention.
BIOORGANIC CHEMISTRY
(2022)