| RRC ID |
68878
|
| 著者 |
Fukuda H, Sato S, Zou T, Higashi S, Takahashi O, Habu M, Sasaguri M, Tominaga K, Takenaka S, Takeuchi H.
|
| タイトル |
Substituent effects of cyclic naphthalene diimide on G-quadruplex binding and the inhibition of cancer cell growth.
|
| ジャーナル |
Bioorg Med Chem Lett
|
| Abstract |
Interaction of cyclic naphthalene diimide derivatives (cNDIs), 1-4, with TA-core and c-myc as G-quartet (G4) DNA was studied under dilute or molecular crowding condition. Binding study for TA-core based on an isothermal titration calorimetry showed that 1-4 has 106 M-1 order of binding affinity with the following order: 1 > 4 > 2 > 3 under both conditions. Meting temperature (Tm) of TA-core obtained from the temperature dependence of circular dichroism spectra shows that TA-core was most stabilized by 4, which is in agreement with the result of PCR stop assay and the stabilization effect for 1-3 was correlated with their binding affinity under dilute condition. 3 showed specific growth inhibition of cancer cell line Ca9-22 at <0.03 μM of IC50, with no inhibitory effect against normal bone marrow cells. 3, which has highest value of ΔH/ΔG, shows the highest inhibition ability for Ca9-22, carrying a highest expression level of telomerase mRNA.
|
| 巻・号 |
50
|
| ページ |
128323
|
| 公開日 |
2021-10-15
|
| DOI |
10.1016/j.bmcl.2021.128323
|
| PII |
S0960-894X(21)00550-3
|
| PMID |
34400300
|
| MeSH |
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Bone Marrow Cells / drug effects
Cell Line, Tumor
Cell Survival / drug effects
Circular Dichroism
Cisplatin / pharmacology
G-Quadruplexes
Humans
Imides / chemistry
Imides / pharmacology*
Keratinocytes / drug effects
Molecular Structure
Naphthalenes / chemistry
Naphthalenes / pharmacology*
Structure-Activity Relationship
|
| IF |
2.572
|
| リソース情報 |
| ヒト・動物細胞 |
Ca9-22(RCB1976) |
