Synthesis and antitumoral activity of novel analogues monastrol–fatty acids against glioma cells

Oliveira, Franciele Saes de; Oliveira, P. M. de; Farias, Luana Machado; Brinkerhoff, Rafael C.; Sobrinho, Rui Carlos M. Alves; Treptow, Tamara M; D'Oca, Caroline R. M.; Marinho, Marcelo Augusto Germani; Hort, Mariana Appel; Horn, Ana Paula; Russowsky, Dennis; D’Oca, Marcelo Gonçalves Montes

doi:10.1039/c8md00169c

“…Such derivatives of compound 22 appeared to be in some cases (linkage to palmitic or stearic acids) up to thirteen times more effective than the unmodified compound. This improved efficacy is likely caused by a better ability to pass through cell membranes owing to the presence of lipophilic fatty acid chains [ 235 ]. The most promising group from the kinesin-5 inhibitors is quinazolines.…”

Section: Kinesins Inhibitorsmentioning

confidence: 99%

Mitotic Poisons in Research and Medicine

Škubník

¹

,

Jurášek

²

,

Ruml

³

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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“…39 The Biginelli reaction is believed by some to be the most important MCR. 40 This MCR (Scheme 1) allows the direct synthesis of bioactive DHMPs (3,4-dihydropyrimidin-2(1H)-ones or -thiones) such as monastrol, piperastrol, and enastron. [41][42][43][44][45][46] It is well known that HPAs possess a very strong acidity in form of protons, which can be changed by varying the chemical composition of the primary structure of the heteropolyanion.…”

Section: Introductionmentioning

confidence: 99%

Nickel salt of phosphomolybdic acid as a bi-functional homogeneous recyclable catalyst for base free transformation of aldehyde into ester

Patel

¹

,

Patel

²

2020

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“…39 The Biginelli reaction is believed by some to be the most important MCR. 40 This MCR (Scheme 1) allows the direct synthesis of bioactive DHMPs (3,4-dihydropyrimidin-2(1H)ones or -thiones) such as monastrol, piperastrol, and enastron. [41][42][43][44][45] HPAs and their derivatives have been previously used to promote the Biginelli reaction; however, in general, only moderate yields were achieved using organic solvents and no mechanistic elucidation was described.…”

Section: Introductionmentioning

confidence: 99%

“… 39 The Biginelli reaction is believed by some to be the most important MCR. 40 This MCR ( Scheme 1 ) allows the direct synthesis of bioactive DHMPs (3,4-dihydropyrimidin-2(1 H )-ones or -thiones) such as monastrol, piperastrol, and enastron. 41–45 …”

Section: Introductionmentioning

confidence: 99%