| 摘要 |
Oligonucleotide analogues of formula (I) and their salts are new, in which B = nucleotide bases, at least one of which is of formula (II); R15 and R16 = H, halogen, 1-10C alkyl, 2-10C alkenyl or alkynyl, NO2, NH2, CN, 1-6C alkylthio or alkoxy, 6-20C aryloxy, SiH3 or CORa, where the alkyl, alkenyl and alkynyl gps. are opt. halogenated or substd., where functional substits. are opt. linked to gps. that enhance intracellular uptake, act as probe labels or interact with hybridised target nucleic acids by binding, crosslinking or cleaving, provided that R15 and R16 are not both H, NO2, NH2, CN or SiH3; Ra = OH, 1-6C alkoxy, 2-20C aryloxy, NH2 or NHT; T = an alkylcarboxy (sic) or alkylamino gp. linked to one or more gps. that enhance intracellular uptake, act as probe labels or interact with hybridised target nucleic acids by binding, crosslinking or cleaving; E and F = H, OH or NH2; R1 = H, 1-18C alkyl, 2-18C alkenyl, alkynyl or alkanoyl, 3-19C alkenoyl or alkynoyl, (6-14C)aryl(1-8C)alkyl, a protecting gp. or P(W)ZZ'; R1a = H, 1-18C alkyl, 2-18C alkenyl, alkynyl or alkanoyl, 3-19C alkenoyl or alkynoyl, (6-14C)aryl(1-8C)alkyl or P(W)ZX; R2 = H, OH, 1-18C alkoxy, 2-6C alkenyloxy, halogen, azido or NH2; A = O, S or CH2; n = 1 or more; W = O, S or Se; V = O, S or NH; Y = O, S, NH or CH2; Y' = O, S, NH, (CH2)m or V(CH2)m; m = 1-18; X = OH or SH; U = OH, SH, SeH, 1-18C alkoxy, 1-18C alkyl, 6-20C aryl, (6-14C)aryl(1-8C)alkyl, NHR3, NR3R4 or (OCH2CH2)pO(CH2)qCH2R5; R3 = 1-18C alkyl, 6-20C aryl, (6-14C)aryl(1-8C)alkyl or (CH2)c(NH(CH2)c)dNR6R6; c = 2-6; d = 0-6; R6 = H, 1-6C alkyl or (1-4C)alkoxy(1-6C)alkyl; R4 = 1-18C alkyl, 6-20C aryl or (6-14C)aryl(1-8C)alkyl; or NR4R4 is a 5- or 6-membered ring opt. contg. another heteroatom (O, S or N); p = 1-100; q = 0-22; R5 = H or a functional gp.; Z and Z' = OH, SH, SeH, 1-22C alkoxy, O(CH2)bNR6R7, 1-18C alkyl, Ar, Ar(1-8C)alkyl, Ar(1-8C)alkoxy, 1-18C alkylthio, NHR3, NR3R4, (OCH2CH2)pO(CH2)qCH2R5 or a gp. that enhances intracellular uptake, acts as a probe label or interacts with a hybridised target nucleic acids by binding, crosslinking or cleaving; b = 1-6; R6 = an undefined substit. and R7 = 1-6C alkyl, or NR6R7 is a 3- to 6-membered ring; Ar = aryl or heteroaryl substd. by 0-3 of COOH, NH2, NO2, 1-4C alkylamino, 1-6C alkoxy, OH, halogen and CN. |
