Title: Marimastat
CAS Registry Number: 154039-60-8
CAS Name: (2
S,3
R)-
N4-[(1
S)-2,2-Dimethyl-1-[(methylamino)carbonyl]propyl]-
N1,2-dihydroxy-3-(2-methylpropyl)butanediamide
Synonyms: N2-[3
S-hydroxy-4-(
N-hydroxyamino)-2
R-isobutylsuccinyl]-L-
tert-leucine-
N1-methylamide
Manufacturers' Codes: BB-2516
Molecular Formula: C15H29N3O5
Molecular Weight: 331.41
Percent Composition: C 54.36%, H 8.82%, N 12.68%, O 24.14%
Literature References: Synthetic matrix metalloproteinase inhibitor (MMPI). Prepn: J. P. Dickens
et al., WO 9402447;
eidem, US 5700838 (1994, 1997 both to British Biotech) and structure-activity study: D. E. Levy
et al., J. Med. Chem. 41, 199 (1998). Improved synthesis: R. J. Davenport, R. J. Watson,
Tetrahedron Lett. 41, 7983 (2000). Clinical study in pancreatic cancer: S. R. Bramhall
et al., J. Clin. Oncol. 19, 3447 (2001); in gastric cancer:
idem et al., Br. J. Cancer 86, 1864 (2002). Review of pharmacology: H. S. Rasmussen, P. P. McCann,
Pharmacol. Ther. 75, 69-75 (1997); and clinical development: A. L. Thomas, W. P. Steward,
Expert Opin. Invest. Drugs 9, 2913-2922 (2000). Review of structure-activity and mechanism of action: M. Whittaker
et al., Chem. Rev. 99, 2735-2776 (1999).
Properties: Soly in water: 1.4 mg/ml.
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic Adjunct; Antimetastatic Agent.