DESIGN AND SYNTHESIS OF TELOMESTATIN DERIVATIVES CONTAINING METHYL OXAZOLE AND THEIR G-QUADRUPLEX STABILIZING ACTIVITIES

DESIGN AND SYNTHESIS OF TELOMESTATIN DERIVATIVES CONTAINING METHYL OXAZOLE AND THEIR G-QUADRUPLEX STABILIZING ACTIVITIES
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DOI:
10.3987/com-10-s(e)85
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发表时间:
2011-03-01
期刊:
影响因子:
0.6
通讯作者:
Nagasawa, Kazuo
Nagasawa, Kazuo
中科院分区:
化学4区
文献类型:
--
作者:
Majima, Satoki;Tera, Masayuki;Nagasawa, Kazuo

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以大环六恶唑为骨架(6OTD),含二甲基恶唑和四甲基恶唑,合成了一种新型的g -四复体配体——l2 - 6m (2)OTD (3b)和l2 - 6m (4)OTD (3c)。这类新的“含甲基恶唑”配体比“不含甲基恶唑”的L2A2-6OTD更有效地稳定各种g -四聚体形成的寡核苷酸(3a)。
Telomestatin derivatives of L2A2-6M(2)OTD (3b) and L2A2-6M(4)OTD (3c), which have a macrocyclic hexaoxazole skeleton (6OTD) containing bis- and tetra-methyl oxazoles, were synthesized as a novel G-quadruplex ligand. This new class of "methyl oxazole containing" ligands was revealed to stabilize various G-quadruplex forming oligonucleotides more potently than "no methyl oxazole containing" L2A2-6OTD (3a).