Abstract：
:Higher-order structures of nucleic acids have become widely noted for their biological consequences and the discovery of an alkylating small molecule for these structures has been of interest due to its therapeutic potential. We previously developed the vinyldiaminotriazine (VDAT)-acridine conjugate as a T-T mismatch alkylating agent. In this report, we focused on the finding of the alkylation to the G-quadruplex (G4) DNA with VDAT-acridine conjugates. The VDAT-acridine conjugates exhibited a considerable alkylation ability to G4 under mild conditions. Moreover, the investigation of properties with the alkylated G4 revealed that alkylation by this conjugate significantly increased the stability of the G4 structure. This study provides a starting point in the further development of selective G4 alkylating small molecules.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Hazemi ME,Onizuka K,Kobayashi T,Usami A,Sato N,Nagatsugi Fdoi
10.1016/j.bmc.2018.05.030subject
Has Abstractpub_date
2018-07-23 00:00:00pages
3551-3558issue
12eissn
0968-0896issn
1464-3391pii
S0968-0896(18)30771-5journal_volume
26pub_type
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