- 5-PHENYL-LH-BENZ0 [E] [1, 4] DIAZEPINE COMPOUNDS SUBSTITUTED WITH AN HYDROXAMIC ACID GROUP AS HISTONE DEACETYLASE INHIBITORS
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Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C=O or CH2 used as antineoplastic agent.
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Page/Page column 14-15
(2009/07/25)
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- Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents
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This study concerns the synthesis of new histone deacetylase inhibitors (HDACi) characterized by a 1,4-benzodiazepine ring used as the cap, joined through an amide function or a triple bond as connection units, to a linear alkyl chain bearing the hydroxamate function as Zn2+-chelating group. Biological tests performed in human acute promyelocytic leukemia NB4 cells showed that new hybrids can induce histone H3/H4 acetylation, growth arrest, and also apoptosis. Notably, chiral compounds exhibit stereoselective activity.
- Guandalini,Cellai,Laurenzana,Scapecchi,Paoletti,Romanelli
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supporting information; experimental part
p. 5071 - 5074
(2009/05/30)
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- A NEW APPROACH TO THE SYNTHESIS OF 2-AMINOMETHYL-3-PHENYL-5-NITROINDOLE
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Bromination of 2-methyl-3-phenyl-5-nitroindoles has given previously unknown 2-bromoethyl-3-phenyl-5-nitroindoles, which were converted by the Delepine reaction into 2-aminomethyl-3-phenyl-5-nitroindoles.One of these (1-methyl-2-aminomethyl-3-phenyl-5-nitroindole) was also obtained by reductive amination of 1-methyl-2-formyl-3-phenyl-5-nitroindole by the Leuckart-Wallach reaction.
- Krichevskii, E. S.,Romanova, O. B.,Grinev, A. N.
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p. 1302 - 1305
(2007/10/02)
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- Process for the preparation of 1,4-benzodiazepine derivatives
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A 1,4-benzodiazepine derivative, or a pharmaceutically acceptable acid salt thereof, of the formula, SPC1 Wherein R1 is hydrogen, halogen, nitro or trifluoromethyl; R2 and R3 are independently hydrogen, halogen, lower alkyl or trifluoromethyl; R4 is lower alkyl, alkenyl, trihaloalkyl, alkoxyalkyl, alkenyloxyalkyl, alkoxyalkoxyalkyl, alkanoyloxyalkyl, cycloalkylalkyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl or a group of the formula EQU1 in which R6 and R7 are independently lower alkyl, and n is an integer of 1 to 4; and R5 is hydrogen or lower alkyl, is obtained by reacting a benzophenone derivative of the formula, SPC2 Wherein R1, R2, R3 and R4 are as defined above, with a 2-isocyanatoacetyl chloride derivative of the formula EQU2 wherein R5 is as defined above.
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