15930-53-7Relevant articles and documents
Synthesis and Biological Evaluation of Benzo[d][1,3]Dioxol-5-yl Chalcones as Antiproliferating Agents
Kamal, Ahmed,Balakrishna, Moku,Loka Reddy, Velatooru,Riyaz, Syed,Bagul, Chandrakant,Satyanarayana, Bethu Murali,Venkateswar Rao, Janapala
, p. 1267 - 1284 (2015)
A series of chalcone derivatives were designed, synthesized, and evaluated for their cytotoxic potential. These molecules have showed promising cytotoxic activity with IC50 values ranging from 5.24 to 63.12 μm. Among them, conjugates 16k, 16m a
A Concise Synthesis of Taiwanin E Using a Michael Initiated Ring Closure Protocol
Harrowven, David C.
, p. 3735 - 3738 (1991)
A rapid entry towards the Podophyllum lignans is described exemplified by a concise regioselective total synthesis of taiwanin E (2). the synthesis features a Michael initiated ring closure sequence to access the key lignan intermediate (11) from the ketodithiolane (10) and the furanone (4).
DNA binding ligands with in vivo efficacy in murine models of bacterial infection: Optimization of internal aromatic amino acids
Buerli, Roland W.,Kaizerman, Jacob A.,Duan, Jian-Xin,Jones, Peter,Johnson, Kirk W.,Iwamoto, Mari,Truong, Kiet,Hu, Wenhao,Stanton, Timothy,Chen, Alfred,Touami, Sofia,Gross, Matthew,Jiang, Vernon,Ge, Yigong,Moser, Heinz E.
, p. 2067 - 2072 (2004)
DNA binding ligands with potent antimicrobial activity against Gram-positive bacteria were further optimized by variation of the internal aromatic amino acids. This modification led to compounds with improved in vivo efficacy in lethal murine models of peritonitis (methicillin-resistant S. aureus, MRSA) and lung infection (S. pneumoniae).
Total synthesis of enantiopure (+)-γ-lycorane using highly efficient Pd-catalyzed asymmetric allylic alkylation
Chapsal, Bruno D.,Ojima, Iwao
, p. 1395 - 1398 (2006)
A highly efficient short total synthesis of (+)-γ-lycorane (>99% ee, 41% overall yield) was achieved by using the asymmetric allylic alkylation in the key step catalyzed by palladium complexes with novel chiral biphenol-based monodentate phosphoramidite l
The effect of carbonyl on the isomerization of a galanthan ring system and total synthesis of (±)-β-lycorane
Liang, Leilei,Li, Ji,Shen, Baochun,Zhang, Yili,Liu, Jianping,Chen, Jingbo,Liu, Dandan
, p. 2767 - 2772 (2021/04/07)
Lycorine-type alkaloids are privileged structures in drug development due to their attractive biological activities. In this paper, the carbonyl on the C ring was proved to have played a critical role in stereoselectivity during the synthesis process, and the galanthan skeleton with acis-B/C ring is more thermodynamically stable in its presence. Furthermore, the total synthesis of (±)-β-lycorane was successfully completed by employing the Michael addition reaction to construct the galanthan skeleton with atrans-B/C ring. This system might be applied to other structural types with similar stereochemistry setting.
DIHYDROCYCLOPENTA-ISOQUINOLINE-SULFONAMIDE DERIVATIVES COMPOUNDS
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Page/Page column 38, (2021/07/02)
The present invention relates to dihydrocyclopenta-isoquinoline-sulfonamide derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use in treating disorders caused by IgE (such as allergic responses, non-allergic mast cell responses or certain autoimmune responses), and in particular disorders caused by the interaction of IgE with the FcεRI receptor.
New method for promoting photosensitive oxidation to remove 1, 2-mercaptoethanol acetal protecting group by utilizing visible light irradiation
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Paragraph 0014-0016, (2021/01/30)
The invention discloses a new method for removing a 1, 2-mercaptoethanol acetal protecting group, and belongs to the field of organic synthetic chemistry. The method comprises the following steps of:under a room-temperature open system, adding a substrate 2-substituted-1, 3-oxo-thio-cyclopentane and a catalytic amount of a photosensitizer Eosin Y into a proper amount of acetonitrile; and performing irradiating with a blue LED lamp for 3 hours while stirring to obtain the corresponding aldehyde compound with favorable yield. The method has the advantages of mild operation conditions, greenness, environmental protection, no harsh water and oxygen removal operation and device, realization of the reaction at room temperature, high substrate conversion rate, simple and easy post-treatment, andprovides a good method for removing the 1, 2-mercaptoethanol acetal protecting group at present.
COMPOUNDS FOR THE INHIBITION OF UNREGULATED CELL GROWTH
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Page/Page column 43, (2020/07/14)
The present invention discloses compounds for inhibition of uncontrolled cell proliferation particularly cancer stem cells. Particularly, the invention relates to compounds of Formula I to XXII for the treatment of cancer.
Visible light photoredox catalyzed deprotection of 1,3-oxathiolanes
Yang, Mingyang,Xing, Zhimin,Fang, Bowen,Xie, Xingang,She, Xuegong
supporting information, p. 288 - 291 (2020/01/13)
An efficient visible light photoredox catalyzed aerobic deprotection of 1,3-oxathiolanes using organic dye Eosin Y as a photocatalyst is disclosed. The deprotection procedure features the use of a metal-free catalyst, mild conditions, a broad range of substrate scope, and good functional group tolerance. 35 examples were tested under the standard conditions and most of them afforded the deprotected products in modest to high yields.
PRODRUGS OF KALLIKREIN INHIBITORS
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Page/Page column 62-63, (2018/05/24)
Disclosed are compounds of formula I, II, and III, and pharmaceutically acceptable salts thereof, which are inhibitors of kallikrein. Also provided are pharmaceutical compositions comprising such a compound, and methods involving use of the compounds and compositions in the treatment and prevention of acquired or hereditary angioedema, or other diseases and conditions characterized by aberrant kallikrein activity. (I) (II) (III)
