Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C28H33N5O2S |
| Molecular Weight | 503.659 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C(N(CCCN)C(=O)C1=CC=C(C)C=C1)C2=NC3=C(C(C)=NS3)C(=O)N2CC4=CC=CC=C4
InChI
InChIKey=SMFXSYMLJDHGIE-UHFFFAOYSA-N
InChI=1S/C28H33N5O2S/c1-18(2)24(32(16-8-15-29)27(34)22-13-11-19(3)12-14-22)25-30-26-23(20(4)31-36-26)28(35)33(25)17-21-9-6-5-7-10-21/h5-7,9-14,18,24H,8,15-17,29H2,1-4H3
AZD4877 was developed by AstraZeneca as a potent inhibitor of the mitotic spindle kinesin, Eg5. AZD4877 participated in clinical trials phase I/II for patients with acute myeloid leukemia, the study was terminated due to lack of efficacy. In addition, the drug was studied in Phase II in patients with previously treated advanced urothelial cancer. However, limited clinical efficacy stops the further development of AZD4877 in urothelial cancer.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent. | 2011 Oct 13 |
|
| Phase I/II multicenter study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of AZD4877 in patients with refractory acute myeloid leukemia. | 2012 Jun |
|
| Phase II study to assess the efficacy, safety and tolerability of the mitotic spindle kinesin inhibitor AZD4877 in patients with recurrent advanced urothelial cancer. | 2013 Aug |
Patents
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Code | English |
| Code System | Code | Type | Description | ||
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19ORU63E06
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DTXSID301026070
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C64522
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10368812
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100000175797
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DB11671
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1176760-49-8
Created by
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ACTIVE MOIETY
