The Azaindole Framework in the Design of Kinase Inhibitors
Abstract
:1. Introduction
Azaindole framework | 4-Azaindole | 5-Azaindole | 6-Azaindole | 7-Azaindole |
---|---|---|---|---|
on-line substructure research a | ||||
Scifinder | ||||
chemical structures | 16,505 | 13,632 | 34,762 | 100,384 |
commercially available | 2517 | 2006 | >2749 | 4273 |
References (patents) | 2158 (1187) | 2923 (961) | 10,497 (1756) | 6576 (2863) |
Reference Evolution from 2003 to 2013 | ||||
Reaxys | ||||
chemical structures | 9701 | 8058 | 27,655 | 58,082 |
commercially available | 707 | 639 | 1116 | 3503 |
References (patents) | 583 (586) | 724 (477) | 3461 (890) | 3951 (2026) |
E molecules | 128 | 150 | 138 | 2300 |
Ambinter | 1105 | 1395 | 4132 | >to 10,000 |
2. ALK Kinase Inhibitors
3. Aurora Kinase Inhibitors
IC50 μM | 22 | 27 | 30 | GSK1070916 |
---|---|---|---|---|
Aurora A | 10,000 | 128 | 6.2 | 1100 |
Aurora B | 26 | 5.7 | 0.51 | 3.2 |
4. Cdc7 Inhibitors
Compound | R | IC50 Cdc7 (μM) | IC50 CDK2 (μM) | Compound | IC50 Cdc7 (μM) | IC50 CDK2 (μM) |
---|---|---|---|---|---|---|
37a | H | 0.98 | 3.7 | 38 | 0.066 | 3.7 |
37b | C6H4 | 0.10 | 0.31 | 39 | 0.66 | 38 |
37c | 2-ClC6H4 | 0.011 | 0.11 | 40 | 0.03 | >80 |
37d | 3-ClC6H4 | 0.16 | >83 | |||
37e | 4-ClC6H4 | 0.33 | 0.06 | |||
37f | 3-pyridinyl | 0.16 | 1.1 | |||
37g | 3-(2-Clpyridinyl) | 0.007 | 0.31 | |||
37h | 4-pyridinyl | 0.25 | 0.16 | |||
37i | 3-furanyl | 0.12 | 0.10 | |||
37j | 3-pyrazole | 0.58 | 0.55 |
5. Check-Point Kinase (CHK1) Inhibitors
6. C-Met Kinase Inhibitors
7. DYRK1A Kinase Inhibitors
8. FAK Inhibitors
9. IKK2 Inhibitors
10. JAK2 Inhibitors
11. KIT/FMS Dual Kinase Inhibitors
12. PAK1 Kinase Inhibitors
13. p38α MAP Kinase Inhibitors
14. PIM Kinase Inhibitors
15. PI3 Kinase Inhibitors
16. B-Raf Kinase Inhibitors
17. Rho Kinase (ROCK) Inhibitors
18. m-TOR Kinase Inhibitors
19. TrkA Kinase Inhibitors
20. Azaindole Binding Mode Analysis
Azaindole Binding to the Hinge Region and Mimicking the Adenine of ATP | 4-Azaindole | 5-Azaindole | 6-Azaindole | 7-Azaindole |
---|---|---|---|---|
Yes | 2WD1 | 4C4E 4C4F 4C4G 4C4H 4C4I 4C4J | None | 1ZYS 2QHM 2QOH 2UVX 2Z60 3BHT 3BHU 3C4C 3C4D 3C4E 3C4F 3CE3 3CTJ 3DJ6 3DK3 3DK6 3DK7 3E87 3ETA 3FQH 3GFW 3GQL 3HDM 3HDN 3JY9 3LJ3 3LVP 3OG7 3RCJ 3ZCL 3ZLS 4AOI 4AWI 4BIC 4BID 4BIE 4FK3 4FV9 4GU6 4HVS 4HW7 4IQ6 4JOA 4K1B 4O91 |
No | 1OZ1 3LVP | 4PMS | None | 2QD9 3EN4 4JG7 |
21. Natural Products as Kinase Inhibitors
22. Conclusions
Acknowledgments
Conflicts of Interest
References
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Mérour, J.-Y.; Buron, F.; Plé, K.; Bonnet, P.; Routier, S. The Azaindole Framework in the Design of Kinase Inhibitors. Molecules 2014, 19, 19935-19979. https://doi.org/10.3390/molecules191219935
Mérour J-Y, Buron F, Plé K, Bonnet P, Routier S. The Azaindole Framework in the Design of Kinase Inhibitors. Molecules. 2014; 19(12):19935-19979. https://doi.org/10.3390/molecules191219935
Chicago/Turabian StyleMérour, Jean-Yves, Frédéric Buron, Karen Plé, Pascal Bonnet, and Sylvain Routier. 2014. "The Azaindole Framework in the Design of Kinase Inhibitors" Molecules 19, no. 12: 19935-19979. https://doi.org/10.3390/molecules191219935