785-56-8Relevant articles and documents
Cyano-and ketone-containing selenoesters as multi-target compounds against resistant cancers
Alonso-Martínez, Francisco-Javier,Benito-Lama, Miguel,Dobiasová, Simona,Domínguez-álvarez, Enrique,Habibullah, Giyaullah,Kincses, Annamária,Nové, Márta,Salardón-Jiménez, Noemi,Sevilla-Hernández, Clotilde,Spengler, Gabriella,Szemerédi, Nikoletta,Viktorová, Jitka
, (2021/09/13)
Fifteen selenocompounds, comprising of eight ketone-containing selenoesters (K1–K8, also known as oxoselenoesters) and seven cyano-containing selenoesters (N1–N7, known also as cyanoselenoesters), have been designed, synthesized, and evaluated as novel anticancer agents. These compounds are derivatives of previously reported active selenoesters and were prepared following a three-step one-pot synthetic route. The following evaluations were performed in their biological assessment: cytotoxicity determination, selectivity towards cancer cells in respect to non-cancer cells, checkerboard combination assay, ABCB1 inhibition and inhibition of ABCB1 ATPase activity, apoptosis induction, and wound healing assay. As key results, all the compounds showed cytotoxicity against cancer cells at low micromolar concentrations, with cyanoselenoesters being strongly selective. All of the oxoselenoesters, except K4, were potent ABCB1 inhibitors, and two of them, namely K5 and K6, enhanced the activity of doxorubicin in a synergistic manner. The majority of these ketone derivatives modulated the ATPase activity, showed wound healing activity, and induced apoptosis, with K3 being the most potent, with a potency close to that of the reference compound. To summarize, these novel derivatives have promising multi-target activity, and are worthy to be studied more in-depth in future works to gain a greater understanding of their potential applications against cancer.
Isoalantolactone derivative, pharmaceutical composition and application thereof
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Paragraph 0014, (2019/02/02)
The invention relates to an isoalantolactone derivative, a pharmaceutical composition and application thereof, especially use of the isoalantolactone derivative shown as formula (I) or a salt pharmaceutical compound thereof in preparation of adjuvant drugs treating cancer, a pharmaceutical composition containing a therapeutically effective amount of isoalantolactone derivative (I) or its salt anda pharmaceutically acceptable carrier or a composition with other anticancer drugs.
Production method of fluvoxamine maleate intermediate (5-methoxy-1-(4-trifluoromethyl benzyl)pentanone)
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Paragraph 0024; 0025; 0029; 0030; 0034; 0035; 0039; 0040, (2018/11/22)
The invention provides a production method of a fluvoxamine maleate intermediate (5-methoxy-1-(4-trifluoromethyl benzyl)pentanone). The production method comprises the following steps of adding 1,2-dichloroethane into 3,5-difluoromethyl benzoic acid, mixing under the low-temperature environment, heating to 60 to 65 DEG C, uniformly stirring, continuing to heat to 80 to 90 DEG C, dripping thionyl chloride, heating and refluxing, stirring to react until no gas overflows, reducing pressure, and distilling, so as to obtain 3,5-bis(trifluoromethyl) benzoyl chloride; adding 1-bromo-4-methyl butyl ether into a solvent, uniformly mixing, adding carbon nanotube-modified magnesium micro-nanoparticle to mix, and dripping benzene diiodide, so as to obtain a Grignard reagent containing the carbon nanotubes; under the ice bath environment, adding the 3,5-bis(trifluoromethyl) benzoyl chloride into a solvent, adding a ferrous chloride catalyst to mix, adding the Grignard reagent containing the carbonnanotubes, and continuing to react, so as to obtain the 5-methoxy-1-(4-trifluoromethyl benzyl)pentanone.