169516-60-3Relevant academic research and scientific papers
CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS
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, (2019/02/13)
The present invention is directed to compounds of the formulae I, II and III as shown below wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
NUCLEOTIDE AND NUCLEOSIDE THERAPEUTIC COMPOSITIONS AND USES RELATED THERETO
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, (2014/08/20)
This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses related thereto. In certain embodiments, the disclosure relates to halogenated nucleosides optionally conjugated to a phosphorus oxide or pharmaceutically acceptable salts thereof. In certain embodiments, the disclosure relates to conjugate compounds or pharmaceutically acceptable salts thereof comprising an amino acid ester or a sphingolipid or derivative linked by a phosphorus oxide to a nucleotide or nucleoside. In certain embodiments, the disclosure contemplates pharmaceutical compositions comprising these compounds for uses in treating infectious diseases, viral infections, and cancer.
ANTIVIRAL AGENTS
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, (2012/01/15)
Compounds of structural formula (I): and pharmaceutically acceptable salts thereof; as defined herein, are described for use in the prevention and/or treatment of HCV infections. Novel compounds of the formula (I) and pharmaceutical formulations containin
Synthesis of 2′-deoxy-2′-fluororibo- and 2′-deoxy- 2′,2′-difluororibonucleosides derived from 6-(het)aryl-7- deazapurines
Perlíková, Pavla,Jornet Martínez, Neus,Slavtínská, Lenka,Hocek, Michal
, p. 8300 - 8310 (2012/09/21)
A series of novel sugar-modified derivatives of cytostatic 6-hetaryl-7-deazapurine ribonucleosides (2′-deoxy-2′-fluororibo- and 2′-deoxy-2′,2-difluororibonucleosides) bearing an aryl or hetaryl group in position 6, was prepared and screened for biological activity. The fluororibo derivatives were prepared by aqueous palladium catalyzed cross-coupling reactions of the corresponding 6-chloro-7-deazapurine 2′-deoxy-2′-fluororibonucleoside 11 with (het)arylboronic acids. The key intermediate 11 was prepared by a six-step sequence from the corresponding arabinonucleoside by selective protection of 3′- and 5′-hydroxyls by acid-labile groups followed by stereoselective SN2 fluorination and deprotection. The difluororibo-series was prepared by non-stereoselective glycosidation of 6-chloro-7-deazapurine with benzoyl-protected 2-deoxy-2,2-difluoro-d-erythro-pentofuranosyl-1-mesylate followed by cross-couplings, separation of anomers and deprotection. The title nucleosides did not show considerable cytostatic or antiviral activity.
Synthesis and anti-HIV-1 activity of 4-substituted-7-(2′-deoxy- 2′-fluoro-4′-azido-β-d-ribofuranosyl)pyrrolo[2,3-d]pyrimidine analogues
Guo, Xiaohe,Li, Yujiang,Tao, Le,Wang, Qiang,Wang, Shuyang,Hu, Weidong,Pan, Zhenliang,Yang, Qinghua,Cui, Yanmei,Ge, Zhaopeng,Dong, Lihong,Yu, Xuejun,An, Haoyun,Song, Chuanjun,Chang, Junbiao
scheme or table, p. 6770 - 6772 (2011/12/21)
Three novel 4-subsituted-7-(2′-deoxy-2′-fluoro-4′-azido- β-d-ribofuranosyl)pyrrolo[2,3-d]pyrimidine analogues were designed, synthesized, and tested for their anti-HIV-1 activity. Initial biological studies indicated that among these pyrrolo[2,3-d]pyrimid
Chemoselective staudinger strategy in the practical, fit for purpose, gram-scale synthesis of an HCV RNA polymerase inhibitor
Campeau, Louis-Charles,O'Shea, Paul D.
scheme or table, p. 57 - 60 (2011/02/25)
The use of a late-stage selective Staudinger reaction in the preparation of the novel HCV RNA polymerase inhibitor is described. Georg Thieme Verlag Stuttgart - New York.
Total synthesis of 2'-deoxy-2'-arafluoro-tubercidin, -toyocamycin, -sangivamycin and certain related nucleosides
Bhattacharya, Birendra K.,Rao, T. Sudhakar,Revankar, Ganapathi R.
, p. 1543 - 1550 (2007/10/02)
A total synthesis of novel nucleosides 2'-deoxy-2'-arafluoro-tubercidin 12, -toyocamycin 23, -sangivamycin 24 and -thiosangivamycin 25 has been accomplished for the first time starting from 4-chloropyrrolopyrimidine 4, and 2-bromo-5-(ethoxymethyleneamino)pyrrole-3,4-dicarbonitrile 16.The sodium-salt glycosylation of secondary amines 4 and 16 with 3,5-di-O-benzoyl-2-deoxy-2-fluoro-α-D-arabinofuranosyl bromide 5 gave the major β-nucleosides 6 and 17 along with minor amounts of α-anomers 7 and 18.Ammonolysis of compound 6 gave the tubercidin analogue 12.The annulation of epimers 17 and 18 furnished the bromotoyocamycin 21 and its α-anomer 22, respectively.Compound 21 was converted into analogues of toyocamycin 23, sangivamycin 24 and thiosangivamycin 25.Similar functional-group manipulation of substrates 7 and 22 provided the α-anomers of compounds 12, 23, 24 and 25.Among the nucleosides tested, the sangivamycin 24 and thiosangivamycin 25 analogues have shown some interesting anti-(human cytomegalovirus) activity and it was observed that compound 25 is more active than compound 24, but less potent than 9-(1,3-dihydroxypropan-2-yloxymethyl)guanine in vitro.
