| 摘要 |
Provided is an oligonucleic acid analog which contains, as at least one structural unit thereof, a modified nucleic acid monomer compound which is a ring-open nucleoside having a cleaved carbon-carbon bond between the 2′ and 3′ positions and a substituent hydroxymethyl group at the 4′ position. When used as siRNA, the oligonucleic acid analog exhibits superior biological stability and target gene expression inhibiting activity. The oligonucleic acid analog can be used in antisense methods, ribozyme methods, and decoy methods, etc., can be used as a nucleic acid aptamer, and can also be used as a nucleic acid probe or molecular beacon, etc., or in genetic diagnostics, etc. |
| 主权项 |
1. A compound represented by the following formula (I): wherein
B represents an optionally substituted heterocyclic group;T1 represents a protective group for a hydroxy group, or a hydrogen atom;T2 represents a phosphorus-containing functional group, a protective group for a hydroxy group, or a hydrogen atom;X represents an oxygen atom, a sulfur atom, —C(E1)(E2)—, —C(═O)—, —C(═S)—, —C(═C(E1)(E2))—, —N(E3)—, or —C(═NE3)—;E1 and E2 each independently represent a hydrogen atom, a halogen atom, an optionally substituted hydroxy group, an optionally substituted C1-6 alkyl group, an optionally substituted C2-6 alkenyl group, or an optionally substituted amino group;E3 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or an optionally substituted C2-6 alkenyl group;R1 represents an optionally substituted C1-6 alkyl group, an optionally substituted C2-6 alkenyl group, or an optionally substituted amino group;R2 represents an optionally substituted hydroxy group, an optionally substituted amino group, a hydrogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted C2-6 alkenyl group, an optionally substituted C2-6 alkynyl group, or a halogen atom; andR3 represents a hydrogen atom, an optionally substituted hydroxy group, an optionally substituted amino group, an optionally substituted C1-6 alkyl group, an optionally substituted C2-6 alkenyl group, an optionally substituted C2-6 alkynyl group, or a halogen atom, or a salt thereof. |
