596103-10-5Relevant articles and documents
Structure-activity relationships of 2-chloro-N6-substituted-4′-thioadenosine-5′-N,N-dialkyluronamides as human A3 adenosine receptor antagonists
Jeong, Lak Shin,Lee, Hyuk Woo,Kim, Hea Ok,Tosh, Dilip K.,Pal, Shantanu,Choi, Won Jun,Gao, Zhan-Guo,Patel, Amit R.,Williams, Wanda,Jacobson, Kenneth A.,Kim, Hee-Doo
, p. 1612 - 1616 (2008/09/19)
On the basis of potent and selective A3 adenosine receptor (AR) antagonist, 2-chloro-N6-(3-iodobenzyl)-4′-thioadenosine-5′-N,N-dimethyluronamide, structure-activity relationships were studied for a series of 5′-N,N-dialkyluronamide d
Structure-activity relationships of 2-chloro-N6-substituted- 4′-thioadenosine-5′-uronamides as highly potent and selective agonists at the human A3 adenosine receptor
Jeong, Lak Shin,Lee, Hyuk Woo,Jacobson, Kenneth A.,Kim, Hea Ok,Shin, Dae Hong,Lee, Jeong A.,Gao, Zhan-Guo,Lu, Changrui,Duong, Heng T.,Gunaga, Prashantha,Lee, Sang Kook,Jin, Dong Zhe,Chun, Moon Woo,Moon, Hyung Ryong
, p. 273 - 281 (2007/10/03)
We have established structure-activity relationships of novel 4′-thionucleoside analogues as the A3 adenosine receptor (AR) agonists. Binding affinity, selectivity toward other AR subtypes, and efficacy in inhibition of adenylate cyclase were studied. Fro
Design, synthesis, and biological activity of N6-substituted-4′-thioadenosines at the human A3 adenosine receptor
Jeong, Lak Shin,Lee, Hyuk Woo,Kim, Hea Ok,Jung, Ji Young,Gao, Zhan-Guo,Duong, Heng T.,Rao, Srikar,Jacobson, Kenneth A.,Shin, Dae Hong,Lee, Jeong A,Gunaga, Prashantha,Lee, Sang Kook,Jin, Dong Zhe,Chun, Moon Woo,Moon, Hyung Ryong
, p. 4718 - 4730 (2007/10/03)
A large series of N6-substituted-4′-thioadenosines were synthesized starting from d-gulonic-γ-lactone, and structure-activity relationships were studied at the human A3 and other subtypes of adenosine receptors (ARs). 2-Chloro-substi
Purine nucleosides
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Page/Page column 6; 17; 27; Sheet 3 of 3, (2010/02/14)
Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R1 is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3′ are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocabonyl, whereas R3 and R3′ do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.
N6-substituted D-4′-thioadenosine-5′-methyluronamides: Potent and selective agonists at the human A3 adenosine receptor
Jeong, Lak Shin,Jin, Dong Zhe,Kim, Hea Ok,Shin, Dae Hong,Moon, Hyung Ryong,Gunaga, Prashantha,Chun, Moon Woo,Kim, Yong-Chul,Melman, Neli,Gao, Zhan-Guo,Jacobson, Kenneth A.
, p. 3775 - 3777 (2007/10/03)
4′-Thio analogues 3-5 of Cl-IB-MECA (2) (Ki = 1.0 ± 0.2 nM at the human A3 adenosine receptor) were synthesized from D-gulono-γ-lactone via 4-thioribosyl acetate 14 as the key intermediate. All synthesized 4′-thionucleosides exhibite