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     Anticancer Agents

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Synthesis and Cytotoxic Activity of Arenecarbaldehyde 2-Pyridinylhydrazone Derivatives
Alessandra Campbell Pinheiro, Sarah Sant’Anna Maranhão, Guilherme Graziany Camelo Carvalho, Augusto César Aragão Oliveira, Cláudia Pessoa, Thaís Cristina Mendonça Nogueira, Cristiane França da Costa, Marcus Vinícius Nora de Souza
Medicine Research    2020, 4 (4): 200016-200016.   DOI: 10.21127/yaoyimr20200016
Abstract252)      PDF (836KB)(386)       Save
Fourteen arenecarbaldehyde 2-pyridinylhydrazone derivatives have been synthesized and evaluated for their cytotoxic potential against four cancer cell lines using the MTT assay. The products were characterized by 1H NMR, 13C NMR, and HRMS, and the cytotoxicity results were expressed as the concentration that induced 50% inhibition of cell growth (IC 50) in μM. The most active compound was 2-pyridinecarbaldehyde 2-pyridinylhydrazone, with an IC50 value of 0.96 μM, which displayed potent and selective activity against the human prostate cancer cell line, PC3, similar to the antineoplastic drug doxorubicin.
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An Effective Inhibitory of Triptolide on Ovarian Cancer
Xiaodi Li, Rui Liu, Ping Wang, and Jun Zhu
Medicine Research    2020, 4 (4): 200017-200017.   DOI: 10.21127/yaoyimr20200017
Abstract176)      PDF (755KB)(311)       Save
This study explores the inhibitory effect of triptolide on ovarian cancer cells through in vitro cell and in vivo animal model experiments. We use the CCK-8 survival rate experiment to determine appropriate concentration of triptolide and the type of cell line including SF9, HEK293, A2780 and Skov-3. Furthermore, the cell invasion and migration of A2780 and Skov-3 cells shows that triptolide had a strong inhibitory effect on ovarian cancer cell line. In addition, flow cytometry is used to detect the apoptosis and cycle of A2780 cells. The results prove that the proliferation of ovarian cancer cell lines is significantly inhibited by triptolide at a 200 nmol/L concentration. Finally, in vivo animal model shows a strong inhibitory effect of triptolide with a 200 nmol/L concentration on ovarian cancer. However, HE staining of animal liver, kidney and ovarian tissue section reveals that there is a stronger effect of 200 nmol/L triptolide on the damage of living organs coming from its toxicity. The result offers a chance for reasonable safety use of triptolide.
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Metal Complexes of Thiosemicarbazones as Potent Anticancer Agents: a Minireview
Yue Zhao, Lijun Wang, Chuanlong Guo, Bo Jiang, Xiangqian Li, Kun Liu, Dayong Shi
Medicine Research    2018, 2 (2): 180009-.   DOI: 10.21127/yaoyimr20180009
Abstract322)   HTML24)    PDF (500KB)(346)       Save

As cancer is one of humanity’s biggest killers in the world, scientists have been looking for different drugs as agents to treat cancer. However, current chemotherapeutics is not sufficiently effective. Thiosemicarbazone complexes of transition metals have attracted wide attention due to a great effect of anticancer activity with different mechanisms including ribonucleotide reductase inhibition, metal dependent radical damage, DNA binding, and inhibition of protein synthesis, and so on. In this minireview, we summarize different metal chelators of thiosemicarbazones and their anticancer mechanisms, which are useful for the development of thiosemicarbazone as anticancer drugs.

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Adverse Reactions and Resistance of Anticancer Drug Cisplatin
Zhonglie Yang, Li Lin, Xiaoyan Peng, Xinyi Yu, Xiaobin Zhang, Hezhong Jiang, and Jiahong Li
Medicine Research    2021, 5 (1): 200022-200022.   DOI: 10.21127/yaoyimr20200022
Abstract286)      PDF (546KB)(372)       Save
Since 1978, cisplatin has become a leading anticancer drug for its high efficacy and unique mechanism of action. As a representative of platinum anticancer drugs, cisplatin has an excellent curative effect and broad application range of cancer. However, its application is limited by high toxicity and drug resistance. This review mainly focuses on adverse reactions and drug resistance of cisplatin.
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Recent Advances on Small-Molecule Tubulin Inhibitors
Xiu-Li Sun, Yin-Rong Xie, Ning Zhang, Cheng-Ting Zi, Xuan-Jun Wang, and Jun Sheng
Medicine Research    2021, 5 (1): 200024-200024.   DOI: 10.21127/yaoyimr20200024
Abstract330)      PDF (778KB)(450)       Save
Microtubules are heterodimers composed of α/β tubulin and make up the cytoskeleton. It plays an important role in maintaining cellular morphology, cell division, signal transduction and other processes. At present, six tubulin inhibitor binding sites have been identified. The inhibitors can be divided into two categories: a type of microtubule polymerization agent includes colchicine site, vinblastine site, maytansine site and prionetin site inhibitors; another category is paclitaxel and laulimalide/peloruside binding site inhibitors are called microtubule depolymerization. Herein, we summarize relevant inhibitors acting on these 6 sites and their research status. With extensive research on tubulin binding sites and inhibitors, anti-tumor tubulin inhibitors will possess very broad clinical prospects.
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Recent Advances on Small-Molecule Epidermal Growth Factor Receptor Inhibitors
Bo-Ya Shi, Ze-Hao Wang, Xuan-Jun Wang Jun Sheng, and Cheng-Ting Zi
Medicine Research    2020, 4 (3): 200011-.   DOI: 10.21127/yaoyimr20200011
Abstract418)      PDF (418KB)(318)       Save
The epidermal growth factor receptor (EGFR) is a kind of cell membrane surface receptor with tyrosine kinase activity, which is closely related to the growth, proliferation, differentiation, apoptosis, metastasis and other processes of tumor cells. Targeting EGFR tyrosine kinase inhibitors has become a hot topic for drug development for treatment of non-small-cell cancer (NSCLC). Herein, we summarized recent advances on the targeted therapeutic drugs for NSCLC in recent years.
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Progress in Antitumor Activity of Diterpenoid Alkaloids
Xiao-Jing Shen, Ting-Ting Zheng, Hong Wang, Jiao Cai, Cheng-Ting Zi, and Jiang-Ping Fan
Medicine Research    2020, 4 (4): 200015-200015.   DOI: 10.21127/yaoyimr20200015
Abstract271)      PDF (887KB)(380)       Save
Diterpenoid alkaloids are a diverse group of natural products with significant structural complexity and bioactivities, including anti-inflammatory, anti-arrhythmia, analgesia, local anesthetic, muscle relaxant, hypotensive, anti-tumor and immune regulation. In this article, we summarized the progress in antitumor activity of diterpenoid alkaloids to provide ideas for medicinal development prospects of antitumor.
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Recent Advances on Interaction Targets for Anticancer Activity of Caffeine
Titi Liu, Chengting Zi, Xuanjun Wang, Jun Sheng, and Huanhuan Xu
Medicine Research    2021, 5 (1): 200020-200020.   DOI: 10.21127/yaoyimr20200020
Abstract261)      PDF (416KB)(433)       Save
Caffeine (1,3,7-trimethylxanthine) is the most frequently ingested neuroactive drug in the world and has enigmatic effects on tumor cells. Convincing evidence from in vitro, animal and human studies suggests that caffeine can inhibit cancer development and progression. Caffeine can easily pass through biological mem-branes and cross the blood-brain barrier, and it is thereby possible to bind to extracellular or intracellular molecules to exert its functions. This review mainly focuses on recent advances in the direct interaction targets of caffeine in the inhibition of malignancies and will hopefully provide valuable insights into the clinical application of caffeine to the treatment of cancers.
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Recent Advances on Anti-skin Cancer Activity of Phytochemicals and Underlying Molecular Mechanisms
Chunxia Gan, Chengting Zi, Jun Sheng, Xuanjun Wang, and Huanhuan Xu
Medicine Research    2021, 5 (2): 210006-210006.  
Abstract261)      PDF (629KB)(247)       Save
Skin is the largest human organ, which always suffered from environmental stresses, as well as extrinsic and intrinsic noxious agents. Although skin can take different protective mechanisms to maintain balance, excessive stresses can disrupt these systems, resulting in the formation of skin cancers, including both melanoma and non-melanoma skin cancers. Phytochemicals are biologically active compounds derived from plants and herbal products, which appear to be beneficial in the battle against cancer as they exhibit anti-cancer effects and are inexpensive, widely available, and well tolerated. Studies have demonstrated that phytochemicals can act on various cellular processes including cell cycle, apoptosis and redox metastasis to inhibit the development and progression of skin cancer. This article mainly focuses on the progress in anti-skin cancer activity of phytochemicals and underlying molecular mechanisms, which will hopefully provide valuable insights into clinical applications of phytochemicals for treatment of skin cancers.
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