106918-31-4Relevant academic research and scientific papers
Folate analogues. 31. Synthesis of the reduced derivatives of 11-deazahomofolic acid, 10-methyl-11-deazahomofolic acid, and their evaluation as inhibitors of glycinamide ribonucleotide formyltransferase
Nair,Murthy,Patil,Kisliuk,Thorndike,Gaumont,Ferone,Dutch,Edelstein
, p. 1277 - 1283 (1989)
The Boon-Leigh procedure, involving condensation of a 6-chloro-5-nitropyrimidine (22) with an α-amino ketone (20 or 21) followed by reduction of the nitro group, cyclization, and L-glutamylation, led to the formation of 11-deazahomofolate (29) and its 10-
PROTEOLYSIS TARGETING CHIMERA (PROTACS) AS DEGRADERS OF SMARCA2 AND/OR SMARCA4
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Page/Page column 54; 56; 76, (2020/05/21)
The present invention encompasses compounds of formula (I) wherein the groups R1,A, G, LK and t have the meanings given in the claims and specification, their use as degraders of SMARCA2 and/or SMARCA4, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
Reductive N-Arylethylation of Aromatic Amines and N-Heterocycles with Enol Ethers
V?gerl, Katharina,Ong, Duc Nghia,Bracher, Franz
, p. 1323 - 1330 (2017/12/26)
A convenient method for N-arylethylation of aromatic amines and heterocycles under mild reductive conditions was developed using (2-methoxyvinyl)(hetero)arenes as building blocks and triethylsilane/trifluoroacetic acid as reducing agent. This protocol is compatible with numerous functional groups, and aliphatic amines are inert due to protonation.
COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY
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Page/Page column 56; 57, (2014/06/24)
The present invention relates to compounds acting both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists, to processes for their preparation, to compositions comprising them, to therapeutic uses and combinations with other pharmaceutical active ingredients.
Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds
Hou, Zengye,Nakanishi, Isao,Kinoshita, Takayoshi,Takei, Yoshinori,Yasue, Misato,Misu, Ryosuke,Suzuki, Yamato,Nakamura, Shinya,Kure, Tatsuhide,Ohno, Hiroaki,Murata, Katsumi,Kitaura, Kazuo,Hirasawa, Akira,Tsujimoto, Gozoh,Oishi, Shinya,Fujii, Nobutaka
supporting information; experimental part, p. 2899 - 2903 (2012/06/01)
Protein kinase CK2 (CK2) is a ubiquitous serine/threonine protein kinase for hundreds of endogenous substrates. CK2 has been considered to be involved in many diseases, including cancers. Herein we report the discovery of a novel ATP-competitive CK2 inhibitor. Virtual screening of a compound library led to the identification of a hit 2-phenyl-1,3,4-thiadiazole compound. Subsequent structural optimization resulted in the identification of a promising 4-(thiazol-5-yl)benzoic acid derivative.
Synthesis and evaluation of a γ-lactam as a highly selective EP2 and EP4 receptor agonist
Xiao, Yufang,Araldi, Gian Luca,Zhao, Zhong,Reddy, Adulla,Karra, Srinivasa,Brugger, Nadia,Fischer, David,Palmer, Elizabeth,Bao, Bagna,Mckenna, Sean D.
, p. 821 - 824 (2008/09/18)
γ-Lactam analogs (2) of EP4 receptor agonists were identified by substitution of the pyrazolidinone ring (1) with a pyrrolidinone ring. Several compounds (such as 2a, 2h) with high potency, selectivity and acceptable PK profiles were discovered. These were assessed in animal models of ovulation induction and bronchoconstriction.
SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Page/Page column 100, (2008/06/13)
The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R" represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.
Samarium(II)-promoted radical spirocyclization onto an aromatic ring
Ohno, Hiroaki,Okumura, Mitsuaki,Maeda, Shin-Ichiro,Iwasaki, Hiroki,Wakayama, Ryutaro,Tanaka, Tetsuaki
, p. 7722 - 7732 (2007/10/03)
Samarium(II)-mediated spirocyclization onto an aromatic ring was achieved by the reaction of methyl 4-(4-oxoalkyl)benzoates with SmI2 in the presence of i-PrOH and HMPA, yielding methyl 1-alkyl-1-hydroxyspiro[4.5]dec-6-ene-8-carboxylates in moderate to high yields. Utilizing this chemistry, spiro[3.5] and -[5.5] systems, and sterically congested spiro[4.5] systems, were easily synthesized. For the successful conversion, appropriate activation of the aromatic ring has proven to be extremely important: while an ester or amide functionality on the aromatic ring can promote the spirocyclization, a sulfonamide substituent causes ortho cyclization.
