Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations
Abstract
:1. Introduction
2. Indole-Based Tubulin Inhibitors
2.1. TMP Analogues
2.2. Arythioindoles
2.3. Aroyindoles
2.4. Fused Indole
2.5. Carbazoles
2.6. Azacarbolines
2.7. Alkaloid Nortopsentin Analogues
2.8. Bis-Indole Derivatives
2.9. Others
3. Conclusions and Perspective
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Drug Name (Company) | Target | Indications | Year (FDA) |
---|---|---|---|
Vincristine (Eli Lilly) | Tubulin | Hodgkin lymphoma | 1963 |
Vinorelbine (Pierre Fabre) | Tubulin | Hodgkin lymphoma | 1994 |
Alectinib (Roche) | ALK | NSCLC | 2015 |
Panobinostat (Novartis) | HDACs | Multiple myeloma | 2015 |
Sunitinib (Pfizer) | VEGFR | Gastrointestinal stromal tumor | 2006 |
Osimertinib (AstraZeneca) | EGFR | NSCLC | 2015 |
Comp. | IC50 (μM) | ||||||
---|---|---|---|---|---|---|---|
HepG2 | A549 | K562 | HCT-8 | H22 | Bel-7402 | LO2 | |
14e | 0.075 ± 0.005 | 0.305 ± 0.026 | 0.055 ± 0.005 | 0.287 ± 0.034 | 0.060 ± 0.015 | 0.080 ± 0.023 | 0.240 ± 0.090 |
Comp. | IC50 (μM) | |||||||
---|---|---|---|---|---|---|---|---|
HeLa | MCF-7 | MDA | PA-1 | HepG2 | PBMC | WI38 | HEK | |
31 | 1.5 ± 0.25 | 5.25 ± 0.31 | 8 ± 0.87 | 24.7 ± 2.61 | 29.7 ± 3.25 | 50 ± 4.8 | 41.5 ± 4.2 | 46.5 ± 3.5 |
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Tang, S.; Zhou, Z.; Jiang, Z.; Zhu, W.; Qiao, D. Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations. Molecules 2022, 27, 1587. https://doi.org/10.3390/molecules27051587
Tang S, Zhou Z, Jiang Z, Zhu W, Qiao D. Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations. Molecules. 2022; 27(5):1587. https://doi.org/10.3390/molecules27051587
Chicago/Turabian StyleTang, Sheng, Zhihui Zhou, Zhiyan Jiang, Wufu Zhu, and Dan Qiao. 2022. "Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations" Molecules 27, no. 5: 1587. https://doi.org/10.3390/molecules27051587