Patent classifications
C07C391/00
Organoselenium compounds, method for producing same, and pharmaceutical uses thereof in particular as antitumor agents
The invention relates to a selenium compound. Said selenium compound has formula (I), where R.sup.1=alkyl; R.sup.2=H, R.sup.4C(=0), R.sup.4OC(=0), a-aminoacyl, CH.sub.3SeCH.sub.2CH.sub.2CH(NH.sub.2)C(=0), CH.sub.3SeCH.sub.2CH.sub.2CH(OH)C(=0); X=OH, OR.sup.3, NH.sub.2, NR.sup.4R.sup.5, -amino acid, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)NH, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)0-; R.sup.3=alkyl; R.sup.4=alkyl, aryl; R.sup.5=H, alkyl, aryl; R.sup.4 and R.sup.5 which can together form a 5- or 6-membered cycloalkyl radical which can comprise a heteroatom; provided that when X=NH-terbutyl, R.sup.2C(=0)CH.sub.3. Said compound can be used as a pharmaceutical substance, in particular as an antitumour substance.
Organoselenium compounds, method for producing same, and pharmaceutical uses thereof in particular as antitumor agents
The invention relates to a selenium compound. Said selenium compound has formula (I), where R.sup.1=alkyl; R.sup.2=H, R.sup.4C(=0), R.sup.4OC(=0), a-aminoacyl, CH.sub.3SeCH.sub.2CH.sub.2CH(NH.sub.2)C(=0), CH.sub.3SeCH.sub.2CH.sub.2CH(OH)C(=0); X=OH, OR.sup.3, NH.sub.2, NR.sup.4R.sup.5, -amino acid, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)NH, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)0-; R.sup.3=alkyl; R.sup.4=alkyl, aryl; R.sup.5=H, alkyl, aryl; R.sup.4 and R.sup.5 which can together form a 5- or 6-membered cycloalkyl radical which can comprise a heteroatom; provided that when X=NH-terbutyl, R.sup.2C(=0)CH.sub.3. Said compound can be used as a pharmaceutical substance, in particular as an antitumour substance.
Deuterated 3,3'-Diselenodipropionic Acid (DSePA) and Its Use as an Anticancer or Radioprotective Agent
The present invention applies to a deuterated derivative of 3,3-diselenodipropionic acid (D-DSePA), an organo-selenium compound and method of synthesis thereof. The invention also provides the method including D-DSePA for the inhibition of the proliferation of human non-small cell lung carcinoma (NSCLC) cells. This compound inhibits the proliferation of A549, H1975 and H3122 cells of NSCLC origin at a much lower concentration than that needed to inhibit the growth of non-cancerous lung fibroblast cells (WI-38 and WI-26 VA4). Further, D-DSePA exhibits additive effect in A549 lung cancer cells while protecting non-cancerous WI38 cells from radiotoxicity.
Deuterated 3,3'-Diselenodipropionic Acid (DSePA) and Its Use as an Anticancer or Radioprotective Agent
The present invention applies to a deuterated derivative of 3,3-diselenodipropionic acid (D-DSePA), an organo-selenium compound and method of synthesis thereof. The invention also provides the method including D-DSePA for the inhibition of the proliferation of human non-small cell lung carcinoma (NSCLC) cells. This compound inhibits the proliferation of A549, H1975 and H3122 cells of NSCLC origin at a much lower concentration than that needed to inhibit the growth of non-cancerous lung fibroblast cells (WI-38 and WI-26 VA4). Further, D-DSePA exhibits additive effect in A549 lung cancer cells while protecting non-cancerous WI38 cells from radiotoxicity.
Method for producing methionine
The invention concerns a method for alkaline hydrolysis of 5-(2-methylmercaptoethyl)hydantoin of formula (1)
##STR00001## or of its seleniated equivalent, 5-(2-methylselenoethyl)hydantoin, into a methionine salt or a selenomethionine salt, respectively, said method being carried out in a basic aqueous medium, in a reactive stripping packed column, as well as a method for producing the methionine and the selenomethionine implementing it.
Method for producing methionine
The invention concerns a method for alkaline hydrolysis of 5-(2-methylmercaptoethyl)hydantoin of formula (1)
##STR00001## or of its seleniated equivalent, 5-(2-methylselenoethyl)hydantoin, into a methionine salt or a selenomethionine salt, respectively, said method being carried out in a basic aqueous medium, in a reactive stripping packed column, as well as a method for producing the methionine and the selenomethionine implementing it.
Use of sulfur and selenium compounds as precursors to nanostructured materials
The presently disclosed subject matter provides processes for preparing nanocrystals, including processes for preparing core-shell nanocrystals. The presently disclosed subject matter also provides sulfur and selenium compounds as precursors to nanostructured materials. The presently disclosed subject matter also provides nanocrystals having a particular particle size distribution.
Use of sulfur and selenium compounds as precursors to nanostructured materials
The presently disclosed subject matter provides processes for preparing nanocrystals, including processes for preparing core-shell nanocrystals. The presently disclosed subject matter also provides sulfur and selenium compounds as precursors to nanostructured materials. The presently disclosed subject matter also provides nanocrystals having a particular particle size distribution.
Small molecule anticancer agents, combinations and uses thereof
The invention relates to methods of treating cell proliferative disorders. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.
Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes
The marine natural product ()-8,15-diisocyano-11(20)-amphilectene, isolated from the Caribbean sponge Svenzea flava, was used as scaffold to synthesize five new products, all of which were tested against laboratory strains of Plasmodium falciparum and Mycobacterium tuberculosis H.sub.37Rv. The scaffold contains two isocyanide units that are amenable to chemical manipulation, enabling them to be elaborated into a small library of sulfur and selenium compounds. The scaffold along with its isothio- and isoselenocyanate analogs has low to sub-micro molar antiplasmodial activity.