102405-32-3Relevant articles and documents
HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME
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Paragraph 00148; 00149, (2015/01/16)
Disclosed are compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein Y, Ra, Ra', Rc, Rf, X2, Rd, Rd', Re, Re', m, and G have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry, useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular and neurodegenerative diseases or disorders.
Chemical synthesis and evaluation of 17α-alkylated derivatives of estradiol as inhibitors of steroid sulfatase
Fournier, Diane,Poirier, Donald
, p. 4227 - 4237 (2011/11/12)
Steroid sulfatase (STS) controls the levels of 3-hydroxysteroids available from circulating steroid sulfates in several normal and malignant tissues. This and the known involvement of active estrogens and androgens in diseases such as breast and prostate cancers thus make STS an interesting therapeutic target. Here we describe the chemical synthesis and characterization of an extended series of 17α-derivatives of estradiol (E2) using different strategies. A variant of the samarium-Barbier reaction with stoichiometric samarium metal and catalytic Kagan reagent formation was used for introducing low reactive benzyl substrates in position 17 of estrone (E1) whereas heterocyclic substrates were metalated and reacted with either the carbonyl or the 17-oxirane of E1. In vitro evaluation of the inhibitory potency of the new compounds against STS identified new inhibitors and allowed a more complete structure-activity relationship study of this family of 17α-derivatives of E2.
CASPASE INHIBITORS BASED ON PYRIDAZINONE SCAFFOLD
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Page/Page column 42-43, (2008/06/13)
The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.
New enzymes and prodrugs for ADEPT
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, (2008/06/13)
The present invention relates to nucleic acid molecules encoding mutant human carboxypeptidase A enzymes, and encoding conjugates of targeting molecules and mutant human carboxypeptidase A enzymes. The invention further relates to vectors and cell lines containing such nucleic acid molecules.
Amine derivatives, processes for their production and their use
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, (2008/06/13)
Compounds of formula I STR1 wherein R1 represents a group of formula STR2 and R2 represents hydrogen or lower alkyl, or R1 and R2 together with the carbon atom to which they are attached represent a group of for
Retinobenzoic acids. 3. Structure-activity relationships of retinoidal azobenzene-4-carboxylic acids and stilbene-4-carboxylic acids
Kagechika,Himi,Namikawa,Kawachi,Hashimoto,Shudo
, p. 1098 - 1108 (2007/10/02)
Alkyl-substituted azobenzene-4-carboxylic acids are potent differentiation inducers of human promyelocytic leukemia cell line HL-60 to mature granulocytes. Their structure-activity relationships are very similar to those of other retinoidal benzoic acids which are generally represented by 4 and named retinobenzoic acids. The structure-activity relationships of azobenzenecarboxylic acids can also be applied to the known retinoid TTNPB (3). Thus, (E)-4-[2-(3,4-diisopropylphenyl)-1-propenyl]benzoic acid (St30 (28)), and (E)-4-[2-(3-tert-butylphenyl)ethenyl]benzoic acid (St40) (29)), the acyclic alkyl analogues of TTNPB, are nearly as active as retinoic acid. Among the oxidatively derived compounds (Az90, Ep series and Ox series) of azobenzene- or stilbenecarboxylic acids, Az90 (71) and Ep80 (61) have strong activities. However, all the bishydroxylated derivatives of TTNPB are inactive, while a diketo analogue Ox580 (69) has only weak potency. The activities of conformationally restricted compounds of TTNPB offer some information on the stereochemistry of the active form of these retinoidal compounds.
New imidazole anti-fungal agents derived from benzothiophene. Part II
Moreno-Manas, Marcial,Cuberes, Ma. Rosa,Palacin, Celia,Raga, Manuel,Castello, Josep M.,Ortiz, Jose A.
, p. 477 - 482 (2007/10/02)
1-thienyl)methyl>-1H-imidazoles 22, 1-thien-3-yl)(thienyl)methyl>-1H-imidazoles 25 and 1-thien-3-yl)methyl>-1H-imidazoles 28 have been synthesized and tested for anti-fungal activity.All compounds showed good activity against a broad spectrum of fungi (yeasts, dermatophytes).
New Methods of Formation of Meta-Substituted Aromatic Compounds
Adams, Julian,Belley, Michel
, p. 3878 - 3881 (2007/10/02)
The addition of organolithium reagents to the oxa tricyclic ketone 1 occurs stereospecifically to produce the corresponding tertiary carbinols 2a-d.When the alcohols 2a-d are treated with TiCl4, ring fragmentation and dehydration occur to produce good yields of 5,6-dihydrobenzaldehydes 3a-d.Oxidation of aldehydes 3a-d then leads to the corresponding meta-substituted benzaldehydes 4a-d.Alternatively, use of the Lewis acid Me2BBr did not stop at the dihydrobenzaldehyde stage.Tautomerization of the diene aldehydes 3a-d produced meta-substituted benzyl alcohols 7a-d or benzyl bromides 8a-d under prolonged reaction times.The addition of silica gel to the reactions accelerated the formation of the benzyl bromides.
