Ombrabulin
Names
IUPAC name
N 1 -{2-Methoxy-5-[(Z )-2-(3,4,5-trimethoxyphenyl)ethen-1-yl]phenyl}-L -serinamide
Systematic IUPAC name
(2S )-2-Amino-3-hydroxy-N -{2-methoxy-5-[(Z )-2-(3,4,5-trimethoxyphenyl)ethen-1-yl]phenyl}propanamide
Other names
AVE-8062; AVE-8062A; AC7700; CS-39-L-Ser.HCl
Identifiers
ChemSpider
UNII
InChI=1S/C21H26N2O6/c1-26-17-8-7-13(9-16(17)23-21(25)15(22)12-24)5-6-14-10-18(27-2)20(29-4)19(11-14)28-3/h5-11,15,24H,12,22H2,1-4H3,(H,23,25)/b6-5-/t15-/m0/s1
N Key: IXWNTLSTOZFSCM-YVACAVLKSA-N
N InChI=1/C21H26N2O6/c1-26-17-8-7-13(9-16(17)23-21(25)15(22)12-24)5-6-14-10-18(27-2)20(29-4)19(11-14)28-3/h5-11,15,24H,12,22H2,1-4H3,(H,23,25)/b6-5-/t15-/m0/s1
Key: IXWNTLSTOZFSCM-YVACAVLKBS
COC1=C(C=C(C=C1)/C=C\C2=CC(=C(C(=C2)OC)OC)OC)NC(=O)[C@H](CO)N
Properties
C 21 H 26 N 2 O 6
Molar mass
402.447 g·mol−1
Except where otherwise noted, data are given for materials in their
standard state (at 25 °C [77 °F], 100 kPa).
Chemical compound
Ombrabulin was an experimental drug candidate discovered by Ajinomoto and further developed by Sanofi-Aventis .[ 1] Ombrabulin is a combretastatin A-4 derivative that exerts its antitumor effect by disrupting the formation of blood vessels needed for tumor growth.[ 2] [ 3]
It was granted orphan drug status by the European Medicines Agency in April 2011.[ 4]
In January 2013, Sanofi said it discontinued development of ombrabulin after disappointing results from phase III clinical trials.[ 5]
^ "Ombrabulin (AVE8062)" . Sanofi-Aventis Oncology.
^ Hori, K; Saito, S; Nihei, Y; Suzuki, M; Sato, Y (1999). "Antitumor effects due to irreversible stoppage of tumor tissue blood flow: evaluation of a novel combretastatin A-4 derivative, AC7700" . Japanese Journal of Cancer Research . 90 (9): 1026–38. doi :10.1111/j.1349-7006.1999.tb00851.x . PMC 5926172 . PMID 10551334 .
^ Hori, K; Saito, S; Kubota, K (2002). "A novel combretastatin A-4 derivative, AC7700, strongly stanches tumour blood flow and inhibits growth of tumours developing in various tissues and organs" . British Journal of Cancer . 86 (10): 1604–14. doi :10.1038/sj.bjc.6600296 . PMC 2746587 . PMID 12085211 .
^ "Orphan Designation EU/3/11/853" . European Medicines Agency. 15 April 2011.
^ "Sanofi has 65 new compounds in development, says R&D chief" .