Aceanthrylene, a non-alternant cyclopenta-fused hydrocarbon, was shown to be weakly mutagenic without S9 and strongly mutagenic with S9 in the Ames Salmonella plate incorporation assay. The compound was most active in strain TA100 (35 revertants/nmole in the presence of 0.3 mg of S9 protein), an...
4 isomeric cyclopenta-derivatives of benz[e]anthracene (benz[a]aceanthrylene, benz[j]aceanthrylene, benz[l]aceanthrylene, and benz[k]acephenanthrylene) were examined for their ability to morphologically transform C3H10T1/2CL8 mouse-embryo fibroblasts. All of these polycyclic aromatic hydrocarbon...
Three novel cyclopenta-fused polycyclic aromatic hydrocarbons were synthesized, benz[d]aceanthrylene,benz[k]aceanthrylene, and benz[j] acephenanthrylene, and evaluated for mutagenic activity in the Ames Salmonella typhimurium plate incorporation assay. The two benzaceanthrylene derivatives were ...
Initial studies on the mutagenicity and metabolism of a novel cyclopenta-PAH, benz[j]aceanthrylene, are reported in the Salmonella bacterial system. The spectrum of activity of benz[j]aceanthrylene over the 5 Ames tester strains is similar to that of benzo[a]pyrene, and the dose-response curves ...
The genotoxicity of the cyclopenta-fused polycyclic aromatic hydrocarbon, benz[l]aceanthrylene (B[l]A), was evaluated in vitro using the L5178YTK+− mouse lymphoma assay and in vivo using the mouse peripheral blood lymphocyte (PBL) culture system. The mutagenicity and sister chromatid exchange (S...
Benz[e]aceanthrylene (B[e]A) and benz[l]aceanthrylene (B[l]A), cyclopenta-fused derivatives of benz[a]anthracene, have been reported to be active bacterial cell and mammalian cell gene mutagens. In this study they were evaluated as skin tumor initiators in both male and female SENCAR mice. Both ...
Cyclopenta-fused polycyclic aromatic hydrocarbons are a class of environmental PAH that have been recently identified. Many of these chemicals have been found to be more active than benzo[a]pyrene in tests for genetic toxicity using bacterial and rodent cells. Benz[l]aceanthrylene, a cyclopenta-...
Benz[j]aceanthrylene (B[j]A), a cyclopenta-fused derivative of benz[a]anthracene, has been reported to be an active bacterial cell and mammalian cell gene mutagen, a morphological transforming agent in C3H10T12CL8 mouse embryo fibroblasts and a mouse lung tumorigen in strain AJ mice. B[j]A was e...
The metabolites of benz[j]aceanthrylene (B[j]A) produced by incubation with liver S9 proteins from rats induced with Aroclor-1254 and phenobarbital have been identified as: trans-B[j]A-1,2-dihydrodiol, B[j]A-9,10-dihydrodiol, B[j]A-11,12-dihydrodiol, and 10-hydroxy-B[j]A. The major metabolite fo...
Benz[j]aceanthrylene, a cyclopentafused polycyclic aromatic hydrocarbon produced in combustion emissions, possesses a bay region and an etheno bridge which may both contribute to the overall genotoxicity of the compound. In order to assess the role of activation at the bay region, the precursor ...
The 4-[N,N-bis(2-chloroethyl)amino]benzoate of 17β-acetamido-5α-androstan-3β-ol, 17β-acetamido-5-androsten-3β-ol, 3β-acetamido-5α-androstan-17β-ol and 3α-acetamido-5β-androstan-17β-ol have been prepared and their antineoplastic effect evaluated against MIA Pa-Ca-2 pancreatic carcinoma...
ObjectiveTo demonstrate that a combination of 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) and Rana catesbeiana ribonuclease-6 (RC6) exerts synergistic cytotoxic effects on human hepatoma cells.
New complex of Ni(II) with p-[N,N-bis(2-chloroethyl)amino]benzaldehyde-4-methyl thiosemicarbazone (CEAB-4-MTSC) have been synthesized and characterized by elemental analysis, IR, electronic, 1H NMR spectroscopy. The crystal structure of the free ligand and complex has been determined by single c...
The p-[N,N-bis(2-chloroethyl)amino]phenylacetic acid esters of hecogenin and aza-homo-hecogenin have been prepared and their antineoplastic activity was evaluated against two basic drug screening systems in rodents, P388 lymphocytic and L1210 lymphoid murine leukemias. Among the compounds tested...
Different inflammatory diseases and allergic reactions are mediated by leukotrienes, which arise from the oxygenation of arachidonic acid catalyzed by 5-lipoxygenase (5-LO). One promising approach for an effective anti-leukotriene therapy is the inhibition of this key enzyme. This study presents...
1-Aryl-5-amino-4-cyanoformimidoyl imidazoles were reacted with acyl and sulfonyl acetonitriles, under mild experimental conditions, leading to imidazo[4,5-b]pyridines and imidazo[4,5-b]pyridine-5-ones. A reaction intermediate could be isolated in the reaction with methyl cyanoacetate, under care...
Novel dipyrido[1,2-a;3′,4′-d]imidazoles 7a–d, dipyrido[1,2-a;4′,3′-d]imidazoles 8a,c and pyrido[1′,2′;1,2]imidazo[4,5-d]pyridazine derivatives 9a–d were synthesized by two pathways: thermal electrocyclic reaction of 3-alkenylimidazopyridine-2-oximes 10 and direct condensation of ethyl gl...
Dipyrido[1,2-a:3′,4′-d]imidazole derivatives can be readily synthetized from various 3-alkyne-2-cyanoimidazo[1,2-a]pyridines via an efficient Grignard reagent-promoted 6-endo-dig cyclization of nitrile to alkynes. A previous optimization of the Sonogashira coupling reaction at C(3) of the 2-cy...
The biliary and urinary elimination of 3H-methadone and its metabolites was quantitatively studied after various routes of administration of the drug to rats. The biliary excretion products consisted largely of the N-demethylated metabolite of methadone, 2-ethylidene-1,5-dimethyl-3,3-diphenylpyr...
In seven methadone-maintained human participants trained to distinguish between a low dose of naloxone (0.15 mg/70 kg, i.m.; i.e., Drug A) and placebo (i.e., Drug B) under an instructed novel-response drug discrimination procedure, the calcium channel blocker isradipine (0–10 mg/70 kg, p.o.; N=...
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