signature=ce284a42999c065c02f649920dbdc0e2,Trans-acting elements for intracellular delivery of nucle...-CSDN博客

这篇博客详细描述了一种由不同核苷酸单元组成的化合物，通过硫代磷酸酯连接，其中包含2'-脱氧核苷酸和其甲基化版本。重点介绍了化合物中正电荷链接的数量与链长的关系，并强调了其可能的应用领域，如生物化学和药物设计。

1. A compound of the formula

(Z)x

wherein:

each Z is independently selected from a 2′-deoxythymidinyl moiety, a 2′-deoxyuridinyl moiety, a 2′-deoxyadenosinyl moiety, a 2′-deoxyinosinyl moiety, a 2′-deoxycytidinyl moiety, a 5-methyl-2′-deoxycytidinyl moiety, a 7-deaza 2′-deoxyguanosinyl moiety, or a corresponding 2′-O-methyl ribonucleosidyl counterpart of the 2′-deoxythymidinyl moiety, the 2′-deoxyuridinyl moiety, the 2′-deoxyadenosinyl moiety, the 2′-deoxyinosinyl moiety, the 2′-deoxycytidinyl moiety, the 5-methyl-2′-deoxycytidinyl moiety, or the 7-deaza 2′-deoxyguanosinyl moiety,

x is an integer from 5-20,

said Z moieties are connected by thiophosphate triester linkages, wherein

3-12 of said thiophosphate triester linkages being positively charged linkages of the formula:

wherein n is an integer from 2 to 6, and

the remainder of said thiophosphate triester linkages are neutral linkages of the formula:

wherein each R1 is C4-C10 alkyl;

provided that when x is 5-6, the number of positively charged linkages is 3, when x is 7-8, the number of positively charged linkages is 3-4, when x is 9-12, the number of positively charged linkages is 3-10, when x is 13-20, the number of positively charged linkages is 4-12.

2. The compound of claim 1, wherein n is an integer from 2 to 6.

3. The compound of claim 1, having the formula (dT)x, (dU)x, (dA)x, (dI)x, (dC)x, d(5-MeC)x, d(7-deazaG)x, (2′-O-methyl U)x, (2′-O-methyl A)x, (2′-O-methyl C)x, (2′-O-methyl 5-MeC)x, (2′-O-me