14594-25-3Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR TREATMENT OF HEDGEHOG PATHWAY ASSOCIATED CONDITIONS
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Page/Page column 32; 33, (2020/01/24)
Provided herein is novel compounds of formula (I), (II), (III), (IV), and (V) as described in the specification, and pharmaceutically acceptable salts, solvates, and prodrugs and compositions thereof, and methods of measuring hedgehog pathway activation in tumor cells, examining tumor cell proliferation, differentiation and apoptosis and using the compounds and pharmaceutical compositions disclosed for treatment of diseases and disorders associated with the hedgehog signaling pathway.
Cycloisomerization of Olefins in Water
Chen, Jason S.,Chun, Yuge,Dang, Vuong Q.,Dushin, Russell G.,Green, Samantha A.,Matos, Jeishla L. M.,Paegel, Brian M.,Piotrowski, David W.,Richardson, Paul,Shenvi, Ryan A.
supporting information, p. 12998 - 13003 (2020/06/02)
Preparative reactions that occur efficiently under dilute, buffered, aqueous conditions in the presence of biomolecules find application in ligation, peptide synthesis, and polynucleotide synthesis and sequencing. However, the identification of functional
Synthesis and Evaluation of Bifunctional Aminothiazoles as Antiretrovirals Targeting the HIV-1 Nucleocapsid Protein
Mori, Mattia,Dasso Lang, Maria Chiara,Saladini, Francesco,Palombi, Nastasja,Kovalenko, Lesia,De Forni, Davide,Poddesu, Barbara,Friggeri, Laura,Giannini, Alessia,Malancona, Savina,Summa, Vincenzo,Zazzi, Maurizio,Mely, Yves,Botta, Maurizio
supporting information, p. 463 - 468 (2019/04/25)
Small molecule inhibitors of the HIV-1 nucleocapsid protein (NC) are considered as promising agents in the treatment of HIV/AIDS. In an effort to exploit the privileged 2-amino-4-phenylthiazole moiety in NC inhibition, here we conceived, synthesized, and tested in vitro 18 NC inhibitors (NCIs) bearing a double functionalization. In these NCIs, one part of the molecule is deputed to interact noncovalently with the NC hydrophobic pocket, while the second portion is designed to interact with the N-terminal domain of NC. This binding hypothesis was verified by molecular dynamics simulations, while the linkage between these two pharmacophores was found to enhance antiretroviral activity both on the wild-type virus and on HIV-1 strains with resistance to currently licensed drugs. The two most interesting compounds 6 and 13 showed no cytotoxicity, thus becoming valuable leads for further investigations.
Synthesis of 5-aminolevulinic acid with nontoxic regents and renewable methyl levulinate
Zai, Yuxia,Feng, Yunchao,Zeng, Xianhai,Tang, Xing,Sun, Yong,Lin, Lu
, p. 10091 - 10093 (2019/04/10)
Synthesis of 5-aminolevulinic acid (5-ALA) was presented with novel bromination of biobased methyl levulinate (ML), followed by ammoniation and hydrolysis. Copper bromide (CuBr2) was employed as the bromination reagent with higher selectivity and activity instead of the conventional liquid bromine (Br2). 5-ALA was obtained in a high yield (64%) and purity (>95%) by optimum design, which is of great potential in industrialization.
Preparation method of 5-haloacetyl propionate
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Paragraph 0045-0049, (2018/10/19)
The invention discloses a preparation method of 5-haloacetyl propionate. Acetylpropionic acid or acetyl propionate and a halogenating agent are taken as raw materials, and the halogenating agent includes NBS (N-Bromosuccinimide), NCS (N-Chlorosuccinimide), ferrous bromide, iron bromide, aluminum bromide, phosphorus tribromide, copper bromide and copper chloride. The acetylpropionic acid or acetylpropionate obtained by hydrolysis of biomass is taken as a raw material, and undergoes a halogenation reaction in the presence of a halogenating agent to synthesize the 5-haloacetyl propionate. The selected raw materials are wide in sources, cheap and readily available; the reaction conditions are mild, and the reaction yield and selectivity are high; moreover, the selected halogenating agent serving as a raw material is less toxic and more environmentally friendly than liquid bromine used in the traditional mercury process, and has a good industrial application prospect.
BIS-(ARYL/HETEROARYL)-METHYLENE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME AND THEIR USE FOR TREATING CANCER
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Page/Page column 27, (2013/07/05)
The present disclosure relates to novel bis-(aryl/heteroaryl)-methylene compounds of formula (I) having vitamin D receptor agonist and histone deacetylase (HDAC) inhibitory efficacy as well as to methods for reducing or inhibiting the proliferation of can
Furanosteroid studies. Improved synthesis of the A,B,C,E-ring core of viridin
Mascall, Kristen C.,Jacobi, Peter A.
supporting information; experimental part, p. 1620 - 1623 (2012/05/04)
The tetracyclic core skeleton of the furanosteroid viridin is prepared in nine steps from readily available materials. The key step in the synthesis is a facile acid-promoted cyclodehydration of an aryloxyketone to prepare the benzofuran moiety. From this intermediate, the known target skeleton is prepared in four steps. This new synthesis is a six-step improvement over the previously reported one.
TRICYCLIC COMPOUNDS AS ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS
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Page/Page column 83, (2010/08/08)
Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and
Substituted 3-Amino-Pyrrolidino-4-Lactams
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Page/Page column 13, (2008/06/13)
The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.
CARBOXYLIC ACID PERI - SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE
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Page/Page column 56-57, (2010/11/08)
Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.
