98453-60-2Relevant academic research and scientific papers
Iron-Catalyzed Synthesis of Dihydronaphthalenones from Aromatic Oxime Esters
Zhang, Youcan,Yin, Zhiping,Wu, Xiao-Feng
, p. 3223 - 3227 (2019/05/10)
Herein, a convenient procedure on iron-catalyzed radical-mediated synthesis of dihydronaphthalenones from oxime esters has been developed. By using iron salt as a green and inexpensive catalyst, various α-aryl oxime esters were transformed into the corresponding dihydronaphthalenones in moderate to good yields with high chemo-selectivities. The reaction proceeds via 1,5-hydrogen atom transfer and then intramolecular radical cyclization sequence. (Figure presented.).
Retinoid receptor subtype-selective modulators through synthetic modifications of RARγ agonists
Alvarez, Susana,Alvarez, Rosana,Khanwalkar, Harshal,Germain, Pierre,Lemaire, Geraldine,Rodriguez-Barrios, Fatima,Gronemeyer, Hinrich,de Lera, Angel R.
supporting information; experimental part, p. 4345 - 4359 (2009/10/17)
A series of retinoids designed to interfere with the repositioning of H12 have been synthesized to identify novel RARγ antagonists based on the structure of known RARγ agonists. The transcriptional activities of the novel ligands were revealed by cell-based reporting assays, using engineered cells containg RAR subtype-selective fusions of the RAR ligand-binding domains with the yeast GAL4 activator DNA-binding domain and the cognate luciferase reporter gene. Whereas none of the ligands exhibited features of a selective RARγ antagonist, some of them are endowed with interesting activities. In particular 24a acts as a pan-RAR agonist that induces at high concentration a higher transactivation potential on RARα than TTNPB and synergizes at low concentration with TTNPB-bound RARα but not RARβ or RARγ. Similarly, 24c synergizes with TTNPB-bound RARγ and exhibits RARα,β antagonist activity. Compounds 24b and 25b are strong RARα,β-selective antagonists without agonist or antagonist activities for RARγ. Compounds 24b and 24c display weak RXR antagonist activity. In addition several pan-antagonists and partial agonist/antagonists have been defined.
DISUBSTITUTED CHALCONE OXIMES HAVING RARγ RETINOID RECEPTOR ANTAGONIST ACTIVITY
-
Page/Page column 19; 21, (2008/06/13)
Compounds of the formula where the variables have the values described in the specification are antagonists of RARγ retinoid receptors.
Disubstituted chalcone oximes as selective agonists of RAR retinoid receptors
-
Page/Page column 23; 24, (2008/06/13)
Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RARγ agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.
5-[PHENYL-TETRAHYDRONAPHTHALENE-2-YL DIHYDRONAPHTHALEN-2-YL AND HETEROARYL-CYCLOPROPYL]-PENTADIENOIC ACID DERIVATIVES HAVING SERUM GLUCOSE REDUCING ACTIVITY
-
Page 13, (2010/02/10)
Compounds of the formula where the variables have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of reducing serum thyroxine levels and transiently increasing triglyceride levels.
NOVEL LIGANDS THAT ARE ANTAGONISTS OF RAF RECEPTORS, PROCESS FOR PREPARING THEM AND USE THEREOF IN HUMAN MEDICINE AND IN COSMETICS
-
Page 24, (2008/06/13)
The invention relates to novel compounds corresponding to formula (I) below: and to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, or alternatively in cosmetic compositions.
O- or S- substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
-
Page column 72, (2010/11/29)
Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
Oxime substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
-
, (2008/06/13)
Compounds of the formula STR1 have retinoid-like or retinoid antagonist-like biological activity.
Acetylenes disubstituted with a 5-amino or substituted 5-amino substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
-
, (2008/06/13)
Compounds of the formula STR1 having retinoid like biological activity.
SUBSTITUENT EFFECTS ON THE RATE OF CARBENE FORMATION BY THE PYROLYSIS OF RIGID ARYL SUBSTITUTED DIAZOMETHANES
Mathur, Naresh C.,Snow, Miles S.,Young, Kent M.,Pincock, James A.
, p. 1509 - 1516 (2007/10/02)
Rate constants for the pyrolysis of 1-diazo-4,4-dimethyl-1,4-dihydronaphtalenes, 4a-4e, have been measured in methanol:6percent triethylamine.In contrast to non-rigid cases, like diphenyldiazomethanes, where all para substituents show a rate increase compared to hydrogen, these rates show a linear Hammett correlation for all para substituents with ?+ = -0.84.This observation is rationalized by a non-linear process for loss of nitrogen leading directly to the ground-state singlet of the carbene, 17.This carbene is then trapped to give ether 11.
