- Benzimidazole derivative BI292 as well as preparation method and application thereof
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The invention discloses a benzimidazole derivative BI292 and a preparation method thereof, and the benzimidazole derivative BI292 is chemically named as 1-[(2R, 4S, 5R)-4-hydroxy-5-(hydroxymethyl) tetrahydrofuran-2-yl]-1H-benzo [d] imidazole-4-carboxylic acid methyl ester. The benzimidazole derivative and the pharmaceutically acceptable salt, the solvate and the hydrate of the benzimidazole derivative have excellent in-vivo and in-vitro anti-tumor activity on MCF-7, SK-BR-3, HCT 116, U-118 MG, U-87 MG and MDA-MB-468, and have a relatively good application prospect in preparation of anti-tumor drugs.
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Paragraph 0019; 0021-0024
(2021/06/09)
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- Benzimidazole derivative BI305 and preparation method and application thereof
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The invention discloses a benzimidazole derivative BI305 and a preparation method thereof, and the chemical name of the benzimidazole derivative BI305 is 1-[tetrahydro-4-hydroxy-5-(hydroxymethyl) furan-2-yl]-N, N-dimethyl-1H-benzo [d] imidazole-4-formamide. The benzimidazole derivative and the pharmaceutically acceptable salt, solvate and hydrate thereof have excellent anti-tumor in-vivo and in-vitro activity on MCF-7, SK-BR-3, HCT 116, U-118 MG, U-87 MG and MDA-MB-468, and have a good application prospect in preparation of anti-tumor drugs.
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Paragraph 0020; 0022-0024
(2021/02/13)
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- Introduction of peptide functions into DNA by nucleic acid peptides, NAPs
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Nucleic acid peptides (NAPs) with a mimetic amino acid side residue at the base position of the nucleotide via an amide bond were synthesized from 3-deoxy-6-O-(4,4′-dimethoxytrityl)allonic acid methyl ester as the common precursor. Furthermore, an NAP with an octapeptide at the C1′ position was synthesized. The peptide-linked NAP exhibits both functions of the oligopeptide part and of the oligonucleotide part. Copyright
- Kawakami, Junji,Wang, Zhong-Ming,Fujiki, Hiroyoshi,Izumi, Satoshi,Sugimoto, Naoki
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p. 1554 - 1555
(2007/10/03)
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- Convenient preparation of 2-deoxy-3,5-di-O-p-toluoyl-α-D-erythro-pentofuranosyl chloride
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By using acetyl chloride as HCl generator, the procedure for the Hoffer preparation of the α-chloro sugar 4a was significantly improved. The α-configuration of the chloro atom was confirmed by using NOE measurement. Sequential transformation of 4a to the β-anomer and to the furfuryl derivative 6 was studied.
- Rolland, Valerie,Kotera, Mitsuharu,Lhomme, Jean
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p. 3505 - 3511
(2007/10/03)
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- Synthesis of (2-deoxy-α- and -β-D-erythro-pentofuranosyl)(thymin-1-yl)alkanes and their incorporation into oligodeoxyribonucleotides. Effect of nucleobase-sugar linker flexibility on the formation of DNA-DNA and DNA-RNA hybrids
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On the basis of modeling studies, the (2-deoxy-α- and β-D-erythro-pentofuranosyl) (thymin-1-yl) alkanes 1a,b and 2a,b were selected as potential conformational probes for altDNA oligonucleotides. A straightforward approach to the synthesis of 1a,b and 2a,b from commercial 2-deoxy-D-ribose (3) and 1-O-methyl-2-deoxy-3,5-di-0-p-toluoyl-D-erythro-pentofuranose (13), respectively, was developed. These nucleoside analogues were converted to the phosphoramidite derivatives 27a,b-30a,b and incorporated into oligonucleotide 31 at predetermined sites and defined internucleotidic motifs. The insertion of 1a,b according to either a (3′ → 5′)- or a (3′ → 3′)-internucleotidic polarity produced oligonucleotides exhibiting a slightly higher affinity for their complementary unmodified DNA sequence than for the corresponding RNA sequence (Table 3). Conversely, the incorporation of 2a into 31 according to a (3′ → 3′)-orientation generated, for the first time, an altDNA oligonucleotide displaying a greater affinity for its complementary unmodified RNA sequence (ΔTm = 6°C) than for the corresponding DNA sequence (ΔTm = 10°C). This hybrid was, however, thermodynamically less stable than the duplex having unmodified α-2′-deoxythymidine similarly incorporated into 31 (ΔΔTm = 3°C).
- Boal, Jila H.,Wilk, Andrzej,Scremin, Carlo L.,Gray, Glenn N.,Phillips, Lawrence R.,Beaucage, Serge L.
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p. 8617 - 8626
(2007/10/03)
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- [(2-deoxy-α- and β-D-erythro-pentofuranosyl)thymin-1-yl] methane derivatives as potential conformational probes for altDNA oligonucleotides
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The previously unknown deoxyribonucleoside analogues 2a,b have been efficiently synthesized from commercial 1-O-methyl-2-deoxy-3,5-di-O-p-toluoyl-D-erythro-pentofuranose. The conversion of these nucleosides to the phosphoramidite derivatives 13a,b and 14a,b for subsequent incorporation into oligodeoxyribonucleotide analogues is also described.
- Scremin,Boal,Wilk,Phillips,Beaucage
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p. 207 - 212
(2007/10/03)
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- Novel DNA Analog for Potential Gene Regulating Agent. A Convenient Synthesis of α-Oligodeoxyribonucleotide Phosphorothioate Bearing 3'-Monophosphate
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α-2'-Deoxyoctathymydilic acid phosphorothioate analog bearing 3'-monophosphate was conveniently synthesized via phosphoramidite method using a riboadenosine attached Teflon-based solid support.The obtained oligomer exhibited enhanced stability toward the digestion by common nucleases.
- Shinozuka, Kazuo,Morita, Tsutomu,Hirota, Yoshiki,Sawai, Hiroaki
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p. 1941 - 1944
(2007/10/02)
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