Reference - Detail
| RRC ID | 68878 |
|---|---|
| Author | Fukuda H, Sato S, Zou T, Higashi S, Takahashi O, Habu M, Sasaguri M, Tominaga K, Takenaka S, Takeuchi H. |
| Title | Substituent effects of cyclic naphthalene diimide on G-quadruplex binding and the inhibition of cancer cell growth. |
| Journal | 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. |
| Volume | 50 |
| Pages | 128323 |
| Published | 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 |
| Altmetric score |
オルトメトリクス指標項目
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| The most frequently cited source | X(Twitter) |
| Total number of mentions | 3 |
| Altmetric score changes over past 6months | 0.0 |
| Resource | |
| Human and Animal Cells | Ca9-22(RCB1976) |