Peptide nucleic acid derivatives with good cell penetration and strong affinity for nucleic acid

A compound of Formula VI:

• wherein,
• R7 is hydrido, N-succinyl, or substituted or non-substituted alkyl radical;
• P1 is selected from hydrido, t-butoxycarbonyl, (9H-fluoren-9-yl)methoxy-carbonyl, substituted or non-substituted benzyloxycarbonyl, and substituted or non-substituted arylsulfonyl radical;
• P2 is selected from hydrido, t-butoxycarbonyl, (9H-fluoren-9-yl)methoxy-carbonyl, substituted or non-substituted benzyloxycarbonyl, substituted alkyloxycarbonyl, substituted or non-substituted alkyl, amidinyl, 1,3-bis(t-butoxy-carbonyl)amidinyl, 1,3-bis-(benzyloxycarbonyl)amidinyl radical;
• and,
• L1 is a linker represented by Formula V:
• wherein,
• Q1 and Qm are substituted or non-substituted methylene radical, and Qm is directly linked to the amino radical;
• Q2, Q3, . . . , and Qm-1 are independently selected from substituted or non-substituted methylene, oxygen, sulfur, and substituted or non-substituted amino radical;
• and,
• m is an integer from 2 to 15.

A compound of Formula IX:

• wherein,
• R10 is hydroxy, substituted or non-substituted alkyloxy, or substituted or non-substituted amino radical;
• P2 is selected from hydrido, t-butoxycarbonyl, (9H-fluoren-9-yl)methoxy-carbonyl, substituted or non-substituted benzyloxycarbonyl, substituted alkyloxycarbonyl, substituted or non-substituted alkyl, amidinyl, 1,3-bis(t-butoxy-carbonyl)amidinyl, 1,3-bis-(benzyloxycarbonyl)amidinyl radical;
• and,
• L1 is a linker represented by Formula V:
• wherein,
• Q1 and Qm are substituted or non-substituted methylene radical, and Qm is directly linked to the amino radical;
• Q2, Q3, . . . , and Qm-1 are independently selected from substituted or non-substituted methylene, oxygen, sulfur, and substituted or non-substituted amino radical;
• and,
• m is an integer from 2 to 15.