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Showing 1 - 5 of 5 results
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Timefurone is a benzopyranone derivative patented by pharmaceutical company Upjohn Co. for the treatment of atherosclerosis. Timefurone mediates the hypolipidemic effect via the reduction of the intracellular synthesis of cholesterol. In preclinical studies, Timefurone significantly lowered low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and total cholesterol in cholesterol-fed male rats and monkeys. Timefurone caused small but significant changes in several clinical chemistry parameters including creatinine, total bilirubin, albumin, glucose, serum glutamic-oxalacetic transaminase, and serum glutamic-pyruvic transaminase in cynomolgus monkeys
Class (Stereo):
CHEMICAL (RACEMIC)
Bromadoline is a selective agonist of a μ-opioid receptor with potent analgesic activity developed by the Upjohn company in the 1970s for pain management.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Steffimycin is a potent inhibitor of DNA dependent-RNA synthesis patented by Upjohn Co. as an antibiotic. Steffimycin interferes with amino acid incorporation mediated by synthetic polyribonucleotides in cell-free bacterial systems. This inhibition is a secondary activity of the antibiotic, which acts primarily as a suppressor of RNA synthesis in bacteria and bacterial cell-free systems. Inhibition of peptide biosynthesis is apparent only at a drug concentration higher than that necessary for inhibition of RNA synthesis in cell-free systems. In addition to antibiotic activity vs certain gram-positive organisms, Steffimycin inhibits the growth of KB cells and several fungi and shows antiviral activity against herpes simplex in mice
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Carzelesin is a cyclopropylpyrroloindole prodrug analogue and DNA minor groove binding agent, with antineoplastic activity. Activation of carzelesin requires hydrolysis of a phenylurethane substituent to form U-76073, followed by ring closure to form the cyclopropyl-containing DNA-reactive U-76074. The formation of the DNA-reactive metabolites from carzelesin was shown to proceed very slowly in phosphate-buffered saline, but to occur rapidly in plasma from mouse, rat, dog, and human and in cell culture medium. Although carzelesin was less potent in terms of in vitro cytotoxicity and in vivo optimal dosage and showed low affinity for binding to DNA, it was therapeutically more efficacious against mouse L1210 leukemia
Class (Stereo):
CHEMICAL (RACEMIC)
Bromadoline is a selective agonist of a μ-opioid receptor with potent analgesic activity developed by the Upjohn company in the 1970s for pain management.