Title: Liarozole
CAS Registry Number: 115575-11-6
CAS Name: 5-[(3-Chlorophenyl)-1
H-imidazol-1-ylmethyl]-1
H-benzimidazole
Synonyms: (±)-5-(
m-chloro-a-imidazol-1-ylbenzyl)benzimidazole
Molecular Formula: C17H13ClN4
Molecular Weight: 308.76
Percent Composition: C 66.13%, H 4.24%, Cl 11.48%, N 18.15%
Literature References: Inhibits cytochrome P450-dependent enzymes involved in steroid biosynthesis and retinoic acid catabolism. Prepn: A. H. M. Raeymaekers
et al., EP 260744;
eidem, US 4859684 (1988, 1989 both to Janssen).
In vivo antitumor activity: R. Van Ginckel
et al., Prostate 16, 313 (1990). Pharmacology and effect on steroid synthesis: J. Bruynseels
et al., ibid., 345; and effect on retinoic acid: R. De Coster
et al., J. Steroid Biochem. Mol. Biol. 43, 197 (1992). Clinical evaluation in prostate cancer: C. Mahler
et al., Cancer 71, 1068 (1993); in psoriasis: P. Dockx
et al., Br. J. Dermatol. 133, 426 (1995); in combination therapy for malignant brain tumors: M. E. Westarp
et al., Onkologie 16, 22 (1993).
Properties: mp 108.2°.
Melting point: mp 108.2°
Derivative Type: Fumarate
CAS Registry Number: 145858-52-2
Manufacturers' Codes: R-85246
Trademarks: Liazal (Janssen)
Molecular Formula: 2C17H13ClN4.3C4H4O4
Molecular Weight: 965.75
Percent Composition: C 57.21%, H 3.97%, Cl 7.34%, N 11.60%, O 19.88%
Derivative Type: Hydrochloride
CAS Registry Number: 145858-50-0
Manufacturers' Codes: R-75251
Molecular Formula: C17H13ClN4.HCl
Molecular Weight: 345.23
Percent Composition: C 59.14%, H 4.09%, Cl 20.54%, N 16.23%
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic.