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Salinosporamide
The salinosporamides are a group of closely related chemical compounds isolated from marine bacteria in the genus ''Salinispora''. They possess a densely functionalized γ-lactam-β-lactone bicyclic core. Salinosporamide A has attracted interest for its potential use in treating various types of cancer. In addition, a variety of synthetic analogs have been prepared. Chemical structures File:Salinosporamide A.svg, Salinosporamide A Salinosporamide A (Marizomib) is a potent proteasome inhibitor being studied as a potential anticancer agent. It entered phase I human clinical trials for the treatment of multiple myeloma, only three years after its discovery in 2003. This marin ... File:Salinosporamide B.svg, Salinosporamide B File:Salinosporamide C.svg, Salinosporamide C File:Salinosporamide D.svg, Salinosporamide D File:Salinosporamide E.svg, Salinosporamide E File:Salinosporamide F.svg, Salinosporamide F File:Salinosporamide G.svg, Salinosporamide G File:Salinosporamide H.svg, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salinosporamide A
Salinosporamide A (Marizomib) is a potent proteasome inhibitor being studied as a potential anticancer agent. It entered phase I human clinical trials for the treatment of multiple myeloma, only three years after its discovery in 2003. This marine natural product is produced by the obligate marine bacteria ''Salinispora tropica'' and ''Salinispora arenicola'', which are found in ocean sediment. Salinosporamide A belongs to a family of compounds, known collectively as salinosporamides, which possess a densely functionalized γ-lactam-β-lactone bicyclic core. History Salinosporamide A was discovered by William Fenical and Paul Jensen from Scripps Institution of Oceanography in La Jolla, CA. In preliminary screening, a high percentage of the organic extracts of cultured ''Salinispora'' strains possessed antibiotic and anticancer activities, which suggests that these bacteria are an excellent resource for drug discovery. ''Salinispora'' strain CNB-392 was isolated from a heat-tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Salinispora
''Salinispora'' is a genus of obligately aerobic, gram-positive, non-acid-fast bacteria belonging to the family of Micromonosporaceae. They are heterotrophic, non-motile, and obligately grow under high osmotic/ ionic-strength conditions. They are the first identified genus of gram-positive bacteria which has a high osmotic/ionic-strength requirement for survival. They are widely abundant in tropical marine sediments and were first identified in 2002. This genus of bacteria has potential biotechnological significance due to their production of novel secondary metabolites which can be used pharmaceutically. There are nine known species that fall within the genus of ''Salinispora'' including the better studied '' S. arenicola'', '' S. tropica'', and '' S. pacifica.'' The clade that initially comprised only ''S. pacifica'' was further interrogated through comparative genomic analyses in 2020 to reveal six additional species. The differentiation of these species is likely the result ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nereus Pharmaceuticals
Nereus Pharmaceuticals was a pharmaceutical company focused on the development of natural products from marine microbial and other natural sources into small molecule human therapeutics. The major disease area addressed by Nereus is cancer. Nereus was purchased by Triphase Research and Development in 2012. Drug discovery Until 2004, Nereus used methods licensed from the University of California, San Diego to retrieve and cultivate marine microorganisms, particularly bacteria in the Actinomycetia class and organisms belonging to Kingdom Fungi. Since 2004, the company has focused on commercializing identified bioactive natural products. As of mid-2007, two compounds were being examined in Phase I clinical trials: NPI-2358 and NPI-0052. * Plinabulin (NPI-2358) is a halimide derivative, halimide itself having been isolated from a member of genus ''Aspergillus''. This compound appears to selectively disrupt tumour vasculature through interaction with microtubules. * NPI-1342 (Aca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Marine Bacteria
Marine prokaryotes are marine bacteria and marine archaea. They are defined by their habitat as prokaryotes that live in marine environments, that is, in the saltwater of seas or oceans or the brackish water of coastal estuaries. All cellular life forms can be divided into prokaryotes and eukaryotes. Eukaryotes are organisms whose cells have a nucleus enclosed within membranes, whereas prokaryotes are the organisms that do not have a nucleus enclosed within a membrane. The three-domain system of classifying life adds another division: the prokaryotes are divided into two domains of life, the microscopic bacteria and the microscopic archaea, while everything else, the eukaryotes, become the third domain. Prokaryotes play important roles in ecosystems as decomposers recycling nutrients. Some prokaryotes are pathogenic, causing disease and even death in plants and animals. [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bicyclic Molecule
In chemistry, a bicyclic molecule () is a molecule that features two joined rings. Bicyclic structures occur widely, for example in many biologically important molecules like α-thujene and camphor. A bicyclic compound can be carbocyclic (all of the ring atoms are carbons), or heterocyclic (the rings' atoms consist of at least two elements), like DABCO. Moreover, the two rings can both be aliphatic (''e.g.'' decalin and norbornane), or can be aromatic (''e.g.'' naphthalene), or a combination of aliphatic and aromatic (''e.g.'' tetralin). Three modes of ring junction are possible for a bicyclic compound: * In spirocyclic compounds, the two rings share only one single atom, the spiro atom, which is usually a quaternary carbon. An example of a spirocyclic compound is the photochromic switch spiropyran. * In fused/condensed bicyclic compounds, two rings share two adjacent atoms. In other words, the rings share one covalent bond, ''i.e.'' the so-called bridgehead atoms are direc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Structural Analog
A structural analog (analogue in modern traditional English; Commonwealth English), also known as a chemical analog or simply an analog, is a compound having a structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is screened for structural analogs of a lead compound. Chemical analogues of il ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Natural Products
A natural product is a natural Chemical compound, compound or chemical substance, substance produced by a living organism—that is, found in nature. In the broadest sense, natural products include any substance produced by life. Natural products can also be prepared by chemical synthesis (both semisynthesis and total synthesis) and have played a central role in the development of the field of organic chemistry by providing challenging synthetic targets. The term natural product has also been extended for commercial purposes to refer to cosmetics, dietary supplements, and foods produced from natural sources without added artificial ingredients. Within the field of organic chemistry, the definition of natural products is usually restricted to organic compounds isolated from natural sources that are produced by the pathways of primary metabolite, primary or secondary metabolite, secondary metabolism. Within the field of medicinal chemistry, the definition is often further restric ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactams
A lactam is a cyclic amide, formally derived from an amino alkanoic acid. The term is a portmanteau of the words ''lactone'' + ''amide''. Nomenclature Greek prefixes in alphabetical order indicate ring size: * α-Lactam (3-atom rings) * β-Lactam (4-atom rings) * γ-Lactam (5-atom rings) * δ-Lactam (6-atom rings) * ε-Lactam (7-atom rings) This ring-size nomenclature stems from the fact that a hydrolyzed α-Lactam leads to an α-amino acid and a β-Lactam to a β-amino acid, ''etc''. Synthesis General synthetic methods exist for the organic synthesis of lactams. Beckmann rearrangement Lactams form by the acid-catalyzed rearrangement of oximes in the Beckmann rearrangement. Schmidt reaction Lactams form from cyclic ketones and hydrazoic acid in the Schmidt reaction. Cyclization of amino acids Lactams can be formed from cyclisation of amino acids via the coupling between an amine and a carboxylic acid within the same molecule. Lactamization is most efficient in this wa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
