- Structure-activity relationships of 2-chloro-N6-substituted-4′-thioadenosine-5′-N,N-dialkyluronamides as human A3 adenosine receptor antagonists
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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
- 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
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p. 1612 - 1616
(2008/09/19)
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- Design, synthesis, and anti-tumor activity of 4′-thionucleosides as potent and selective agonists at the human A3 adenosine receptor
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On the basis of potent and selective binding affinity of Cl-IB-MECA to the human A3 adenosine receptor, its 4′-thioadenosine derivatives were efficiently synthesized starting from D-gulonic γ -lactone. Among compounds tested, 2-chloro-N6/
- Jeong, Lak Shin,Lee, Hyuk Woo,Kim, Hea Ok,Jung, Ji Young,Gunaga, Prashantha,Lee, Sang Kook,Lee, Eun-Jin,Chun, Moon Woo,Gao, Zhan-Guo,Jacobson, Kenneth A.,Moon, Hyung Ryong
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p. 1565 - 1568
(2008/09/21)
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- Structure-activity relationships of 2-chloro-N6-substituted- 4′-thioadenosine-5′-uronamides as highly potent and selective agonists at the human A3 adenosine receptor
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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
- 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
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p. 273 - 281
(2007/10/03)
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- D-4′-thioadenosine derivatives as highly potent and selective agonists at the human A3 adenosine receptor
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4′-Thionucleoside derivatives as potent and selective A3 adenosine receptor agonists were synthesized, starting from D-gulono-γ- lactone via D-thioribosyl acetate as a key intermediate, among which the 2· chloro-N6-methyladenosine-5′
- Lee, Hyouk Woo,Shin, Dae Hong,Jeong, Ji Young,Kim, Hea Ok,Chun, Moon Woo,Melman,Gao,Jacobson, Kenneth A.,Jeong, Lak Shin
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p. 607 - 609
(2008/02/03)
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- Purine nucleosides
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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.
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Page/Page column 6; 17; 27-28; Sheet 3 of 3
(2010/02/14)
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- N6-substituted D-4′-thioadenosine-5′-methyluronamides: Potent and selective agonists at the human A3 adenosine receptor
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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
- 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.
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p. 3775 - 3777
(2007/10/03)
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