- Nucleoside analogs useful as PRMT5 inhibitors
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The invention relates to the technical field of biological medicines, and particularly discloses a nucleoside analogue used as a PRMT5 inhibitor. According to the nucleoside analogue as shown in the formula (I) or the pharmaceutically acceptable salt of the nucleoside analogue, the nucleoside analogue or the pharmaceutically acceptable salt of the nucleoside analogue shows relatively high inhibition on the activity of PRMT5 and can be used for preventing and/or treating PRMT5-mediated diseases, and the PRMT5-mediated diseases comprise cell abnormal proliferative diseases.
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- Tumor immunity compound and application thereof
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Disclosed are a tumor immunity compound and an application thereof. The invention discloses a compound as shown in the formula (I), optical isomers thereof, and pharmaceutically acceptable salts thereof, and an application of the compound as an STING agonist.
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Paragraph 0539; 0568-0571
(2020/07/14)
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- Syntheses of cyclopentyl nucleoside (?)-neplanocin A through tetrazole-fragmentation from cyanophosphates
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We recently reported a novel synthetic method for five-membered unsaturated cyclic compounds from ketones involving cyanophosphates (CPs) under neutral conditions, in which alkylidene carbenes generated through tetrazole-fragmentation undergo [1,5]-C–H in
- Yoneyama, Hiroki,Uemura, Kenji,Usami, Yoshihide,Harusawa, Shinya
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p. 2143 - 2150
(2018/03/26)
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- Structure-Activity Relationships of Neplanocin A Analogues as S -Adenosylhomocysteine Hydrolase Inhibitors and Their Antiviral and Antitumor Activities
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On the basis of the potent inhibitory activity of neplanocin A (1) against S-adenosylhomocysteine (AdoHcy) hydrolase, we analyzed the comprehensive structure-activity relationships by modifying the adenine and carbasugar moiety of 1 to find the pharmacoph
- Chandra, Girish,Moon, Yang Won,Lee, Yoonji,Jang, Ji Yong,Song, Jayoung,Nayak, Akshata,Oh, Kawon,Mulamoottil, Varughese A.,Sahu, Pramod K.,Kim, Gyudong,Chang, Tong-Shin,Noh, Minsoo,Lee, Sang Kook,Choi, Sun,Jeong, Lak Shin
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p. 5108 - 5120
(2015/07/02)
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- Structure based medicinal chemistry approach to develop 4-methyl-7-deazaadenine carbocyclic nucleosides as anti-HCV agent
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The structure-based approaches were implemented to design and rationally select the molecules for synthesis and anti-HCV activity evaluation. The systematic structure-activity relationships of previously discovered molecules (types I, II, III) were analyz
- Thiyagarajan, Anandarajan,Salim, Mohammed T.A.,Balaraju, Tuniki,Bal, Chandralata,Baba, Masanori,Sharon, Ashoke
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p. 7742 - 7747
(2013/02/22)
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- CYCLOPENTENOL NUCLEOSIDE COMPOUNDS, INTERMEDIATES FOR THEIR SYNTHESIS AND METHODS OF TREATING VIRAL INFECTIONS
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The present invention relates to compounds according to the structure (I), Where B is formula (Ia), formula (Ib) or formula (Ic); A is H, OR2 or halogen (F, Cl, Br, I, preferably F or Br, more preferably F); A' is H, OR2 or halogen (F, Cl, Br, I, preferably F or Br, more preferably F); A" is H or OR1, with the proviso that when A' is OR , A is H; and when A is OR2 , A' is H; X is C-R3 or N; Y is C-R3 or N; preferably X or Y is N and X and Y are not both simultaneously N; R3 is H or C1-C3 alkyl; D is H or NHR2; E is absent or H; G is O or NHR2; J is N or C-R4; K is N or C-H; R4 is H, halogen (F, Cl, Br, I), CN, -C(=O)NH2, NH2, NO2, -C=C-H (cis or trans) or -C≡C-H; Ra is H or CH3; Each R1 is independently H, an acyl group, a C1 - C20 alkyl or ether group, a phosphate, diphosphate, triphosphate, phosphodiester group; Each R2 is independently H, an acyl group, a C1 - C20 alkyl or ether group; and Pharmaceutically acceptable salts, solvates or polymorphs thereof.
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Page/Page column 50
(2008/06/13)
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- Synthesis of cyclopentenyl carbocyclic nucleosides as potential antiviral agents against orthopoxviruses and SARS
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A practical and convenient methodology for the synthesis of chiral cyclopentenol derivative (+)-12a has been developed as the key intermediate that was utilized for the synthesis of biologically active carbocyclic nucleosides. The selective protection of
- Cho, Jong Hyun,Bernard, Dale L.,Sidwell, Robert W.,Kern, Earl R.,Chu, Chung K.
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p. 1140 - 1148
(2007/10/03)
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- An improved approach to chiral cyclopentenone building blocks. Total synthesis of pentenomycin I and neplanocin A
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An improved approach to enantiomerically pure hydroxylated cyclopentenones is reported here, which involves intramolecular nitrone cycloaddition of sugar-derived chiral pent-4-enals and hex-5-en-ones-2 followed by N-O bond cleavage, quaternization of the amine thus produced, and finally oxidative elimination of the amino group. Synthesis of pentenomycin I and neplanocin A is described following this methodology.
- Gallos, John K.,Stathakis, Christos I.,Kotoulas, Stefanos S.,Koumbis, Alexandros E.
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p. 6884 - 6890
(2007/10/03)
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- Synthesis of (-)-Neplanocin A via C-H Insertion of Alkylidenecarbene
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(-)-Neplanocin A, a naturally occurring carbocyclic nucleoside was synthesized via C-H insertion reaction of the alkylidenecarbene, which was generated by the reaction of lithiotrimethylsilyldiazomethane and the ketone derived from D-ribose.
- Ohira, Susumu,Sawamoto, Tsukasa,Yamato, Masatoshi
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p. 1537 - 1538
(2007/10/02)
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- Synthesis and Phosphodiesterase Activity of Carboxylic Acid Mimetics of Cyclic Guanosine 3',5'-Monophosphate
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Synthetic analogs of the natural product griseolic acid in which a guanine base is substituted for the adenine have been prepared.The best of these compounds inhibits a cyclic guanosine 3',5'-monophosphate (cGMP) phosphodiesterase preparation with an IC50
- Tulshian, Deen,Czarniecki, Michael,Doll, Ronald J.,Ahn, Ho-Sam
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p. 1210 - 1220
(2007/10/02)
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