- A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase
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HA14-1 is a Bcl-2 inhibitor that is widely used for studies of apoptosis. In the course of searching for a ceramide glucosyltransferase inhibitor that catalyzes the first glycosylation step of glycosphingolipid synthesis, we unexpectedly found that HA-14-1 also has the ability to inhibit ceramide glucosyltransferase. The IC50 value of HA14-1 against ceramide glucosyltransferase is 4.5μM, which is lower than that reported for Bcl-2 in vitro. Kinetic analyses revealed that HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively.
- Niino, Satomi,Nakamura, Yutaka,Hirabayashi, Yoshio,Nagano-Ito, Michiyo,Ichikawa, Shinichi
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Read Online
- First report of the application of simple molecular complexes as organo-catalysts for Knoevenagel condensation
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A series of molecular complexes have been designed, synthesized and used as organo-catalysts for the first time for very efficient Knoevenagel condensation. Molecular complexes are thermally stable, easily recyclable, and have a low cost of preparation. T
- Panja, Sumit Kumar,Dwivedi, Nidhi,Saha, Satyen
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p. 65526 - 65531
(2015/08/18)
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- Synthesis of 2-amino-3-cyano-4H-chromen-4-ylphosphonates and 2-amino-4H-chromenes catalyzed by tetramethylguanidine
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Synthesis of 2-amino-4H-chromen-4-ylphosphonates and 2-amino-4H-chromenes has been accomplished by the reaction of salicylaldehyde, malononitrile, dialkyl/diphenylphosphites catalyzed by 1,1,3,3-tetramethylguanidine (TMG) under neat conditions at room tem
- Kalla, Reddi Mohan Naidu,Byeon, Seong Jin,Heo, Min Seon,Kim, Il
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p. 10544 - 10551
(2013/11/19)
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- Electrocatalytic chain transformation of salicylaldehyde and CH acids into substituted 4H-chromenes
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Electrochemically initiated catalytic chain transformation of salicylaldehydes and CH acids containing the cyano group in an ethanolic solution in an undivided cell produced substituted 4H-chromenes in 85-95% yields.
- Feducovich,Elinson,Dorofeev,Gorbunov,Nasybullin,Stepanov,Nikishin
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experimental part
p. 595 - 600
(2009/05/15)
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- The synthesis of new, selected analogues of the pro-apoptotic and anticancer molecule HA 14-1
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A new and versatile strategy has been developed towards HA 14-1 analogues, selectively modified on position 4 and/or on the primary amine function. An important aspect was the appropriate selection of the phenol protective group in the 5-bromosalicylaldeh
- Grée, Danielle,Vorin, Samuel,Manthati, Vijay L.,Caijo, Frédéric,Viault, Guillaume,Manero, Florence,Juin, Philippe,Grée, René
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p. 3276 - 3278
(2008/09/20)
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- Electrochemically induced chain transformation of salicylaldehydes and alkyl cyanoacetates into substituted 4H-chromenes
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Electrolysis of salicylaldehydes and alkyl cyanoacetates in ethanol in an undivided cell in the presence of sodium bromide results in the formation of substituted alkyl 2-amino-4-(1-cyano-2-alkoxy-2-oxoethyl)-4H-chromene-3-carboxylates in 85-95% yields.
- Elinson, Michail N.,Dorofeev, Alexander S.,Feducovich, Sergey K.,Gorbunov, Sergey V.,Nasybullin, Ruslan F.,Stepanov, Nikita O.,Nikishin, Gennady I.
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p. 7629 - 7633
(2007/10/03)
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- Potassium exchanged layered zirconium phosphate as catalyst in the preparation of 4H-chromenes
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Substituted 4H-chromenes were easily prepared by reaction of salicylaldehydes and ethylcyanoacetate in solvent free conditions using potassium exchanged layered zirconium phosphate as catalyst.
- Curini, Massimo,Epifano, Francesco,Chimichi, Stefano,Montanari, Francesca,Nocchetti, Morena,Rosati, Ornelio
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p. 3497 - 3499
(2007/10/03)
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- Reactions of salicylaldehydes with alkyl cyanoacetates on the surface of solid catalysts: Syntheses of 4H-chromene derivatives
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Substituted 4H-chromene derivatives are a new class of compounds that bind Bcl-2 protein and induce apoptosis in tumor cells. Here we report an efficient synthetic method for the preparation of these compounds from salicylaldehyde derivatives and alkyl cyanoacetates under solid-phase catalysis. (C) 2000 Elsevier Science Ltd.
- Yu,Aramini,Germann,Huang
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p. 6993 - 6996
(2007/10/03)
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