Efficient synthesis and cytotoxicity of novel microtubule-stabilizing agent ceratamine A analogues

Tao, Lulu; Pan, Xuan; Ji, Ming; Chen, Xiaoguang; Liu, Zhanzhu

doi:10.1016/j.tet.2017.03.008

Cited by 7 publications

(2 citation statements)

References 18 publications

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“…Given by that simple structure, they are able to cross the blood-brain barrier and act directly in the brain, which could be utilized, for example, in the treatment of Alzheimer’s disease. At present, syntheses of ceratamine analogues have been performed in order to develop novel substances with improved antiproliferative properties [ 159 ].…”

Section: Microtubule Inhibitorsmentioning

confidence: 99%

“…One of the most recent studies in this field is a study of Tao et al (2017), who confirmed the importance of the methyl group at the C-14 and C-16 position. Derivative 15d showed relatively good anticancer activity with the IC 50 = 23 µM (IC 50 of 15a was equal to 26.5 µM) in cells from lung carcinoma (A549 cell line) [ 159 ]. A much more significant increase in the antiproliferative activity was observed for derivative 15e (IC 50 in A549 cells of 8.56 µM) with a benzyl group at the N-7 and substitution with three methoxy groups on the benzene ring [ 160 ].…”

Section: Microtubule Inhibitorsmentioning

confidence: 99%

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Mitotic Poisons in Research and Medicine

et al. 2020

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Cancer is one of the greatest challenges of the modern medicine. Although much effort has been made in the development of novel cancer therapeutics, it still remains one of the most common causes of human death in the world, mainly in low and middle-income countries. According to the World Health Organization (WHO), cancer treatment services are not available in more then 70% of low-income countries (90% of high-income countries have them available), and also approximately 70% of cancer deaths are reported in low-income countries. Various approaches on how to combat cancer diseases have since been described, targeting cell division being among them. The so-called mitotic poisons are one of the cornerstones in cancer therapies. The idea that cancer cells usually divide almost uncontrolled and far more rapidly than normal cells have led us to think about such compounds that would take advantage of this difference and target the division of such cells. Many groups of such compounds with different modes of action have been reported so far. In this review article, the main approaches on how to target cancer cell mitosis are described, involving microtubule inhibition, targeting aurora and polo-like kinases and kinesins inhibition. The main representatives of all groups of compounds are discussed and attention has also been paid to the presence and future of the clinical use of these compounds as well as their novel derivatives, reviewing the finished and ongoing clinical trials.

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Section: Microtubule Inhibitorsmentioning

confidence: 99%

Section: Microtubule Inhibitorsmentioning

confidence: 99%

Mitotic Poisons in Research and Medicine

et al. 2020

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Transition‐Metal‐Catalyzed Alkyne Hydroarylation with Arylmetals and Aryl Halides

Yamamoto

2020

Organic Reactions

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The aryl alkene is one of the most ubiquitous molecular scaffolds found in diverse natural products, materials, and pharmaceuticals. Aryl alkenes are also essential synthetic intermediates in both industrial and academic laboratories. Nevertheless, traditional preparative methods have fundamental disadvantages, such as the necessity of lengthy synthetic operations and difficulty in the site‐ and stereoselective construction of multiply substituted derivatives. The development of a more straightforward and site‐ and stereoselective method to prepare aryl alkenes has therefore been an important objective in organic chemistry. A particularly attractive method to synthesize aryl alkenes is transition‐metal‐catalyzed alkyne hydroarylation using aryl donor reagents, which proceeds through the formal addition of Ar–H across the carbon–carbon triple bond of an alkyne. This chapter provides an overview of alkyne hydroarylations catalyzed by homogeneous metal catalysts. The mechanism, selectivity, scope and limitations, and experimental conditions of transition‐metal‐catalyzed alkyne hydroarylations are surveyed according to the aryl donor reagent and its role in the reaction; namely, (1) alkyne hydroarylations using arylmetal reagents (alkyne carbometallation/protonation), and (2) alkyne hydroarylations using aryl halides (reductive Heck reaction).

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Tetrahydroazepines with an annulated five-membered heteroaromatic ring

Danyliuk

Вовк²

2022

Chem Heterocycl Comp

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Efficient synthesis and cytotoxicity of novel microtubule-stabilizing agent ceratamine A analogues

Cited by 7 publications

References 18 publications

Mitotic Poisons in Research and Medicine

Mitotic Poisons in Research and Medicine

Transition‐Metal‐Catalyzed Alkyne Hydroarylation with Arylmetals and Aryl Halides

Tetrahydroazepines with an annulated five-membered heteroaromatic ring

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