scholarly journals Further observations on the oestrogenic activity of synthetic polycyclic compounds

1936 ◽  
Vol 121 (821) ◽  
pp. 133-141 ◽  
Keyword(s):  
Ovariectomized Rats ◽  
Straight Chain ◽  
New Members ◽  
Polycyclic Compounds ◽  
Negative Results ◽  
Highly Active ◽  
Polycyclic Aromatic ◽  
Allyl Compound ◽  
Branched Chain ◽  
New Compounds

In a former communication (Cook, Dodds, Hewett, and Lawson, 1934) we recorded the oestrogenic activity of a number of polycyclic aromatic and hydroaromatic compounds. The most active substances were found among a series of diols related to the carcinogenic hydro­carbon, 1 : 2 : 5 : 6-dibenzanthracene. We have now extended our investi­gation to seven new members of this series and have also examined a variety of diols of analogous structure, but containing other ring systems. Table I summarizes the results obtained in tests for oestrogenic activity carried out with 9: 10-dihydroxy-9: 10-dialkyl-9: 10-dihydro-1: 2: 5: 6- dibenzanthracenes. In none of the new compounds has the activity exceeded that of the most potent compound previously described, namely, the di- n -propyl derivative in this series. Among the straight-chain dialkyl compounds this di- n -propyl compound represents a peak of activity in a series of which the first (methyl) and higher ( n -amyl, n -hexyl) members are inactive. Two branched-chain compounds ( iso -propyl, iso -butyl) are fairly highly active, but show diminished activity by comparison with the corresponding straight-chain isomerides. This is particularly marked for the iso -propyl compound, which is about ten times less active than the n -propyl compound. In view of the high order of activity of the n -propyl compound, it is remarkable that the allyl compound has given negative results when injected into ovariectomized rats in 10 mg. doses.

scholarly journals Direct Amidation to Access 3-Amido-1,8-Naphthalimides Including Fluorescent Scriptaid Analogues as HDAC Inhibitors

Cells ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1505
Author(s):  
Kyle N. Hearn ◽  
Trent D. Ashton ◽  
Rameshwor Acharya ◽  
Zikai Feng ◽  
Nuri Gueven ◽  
...  
Keyword(s):  
Optical Properties ◽  
Histone Deacetylase ◽  
Good Yield ◽  
Hdac Inhibitors ◽  
Selective Inhibitor ◽  
Imaging Studies ◽  
Highly Active ◽  
Theranostic Applications ◽  
New Compounds ◽  
Direct Amidation

Methodology to access fluorescent 3-amido-1,8-naphthalimides using direct Buchwald–Hartwig amidation is described. The protocol was successfully used to couple a number of substrates (including an alkylamide, an arylamide, a lactam and a carbamate) to 3-bromo-1,8-naphthalimide in good yield. To further exemplify the approach, a set of scriptaid analogues with amide substituents at the 3-position were prepared. The new compounds were more potent than scriptaid at a number of histone deacetylase (HDAC) isoforms including HDAC6. Activity was further confirmed in a whole cell tubulin deacetylation assay where the inhibitors were more active than the established HDAC6 selective inhibitor Tubastatin. The optical properties of these new, highly active, compounds make them amenable to cellular imaging studies and theranostic applications.

scholarly journals The Peroxisomal Acyl-CoA Thioesterase Pte1p fromSaccharomyces cerevisiaeIs Required for Efficient Degradation of Short Straight Chain and Branched Chain Fatty Acids

2006 ◽  
Vol 281 (17) ◽  
pp. 11729-11735 ◽  
Author(s):  
Isamu Maeda ◽  
Syndie Delessert ◽  
Seiko Hasegawa ◽  
Yoshiaki Seto ◽  
Sophie Zuber ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Straight Chain ◽  
Branched Chain Fatty Acids ◽  
Branched Chain ◽  
Chain Fatty Acids

scholarly journals The homogeneous unimolecular decomposition of gaseous alkyl nitrites - IV—The decomposition of Iso -propyl nitrite

1935 ◽  
Vol 151 (874) ◽  
pp. 685-693 ◽  
Keyword(s):  
Activation Energy ◽  
Thermal Decomposition ◽  
Pressure Change ◽  
Methyl Ethyl ◽  
Unimolecular Decomposition ◽  
Decomposition Rates ◽  
Straight Chain ◽  
Alkyl Nitrites ◽  
Branched Chain ◽  
Reaction Vessels

It has already been shown that the first three straight chain members of the nitrite homologous series, i. e ., methyl, ethyl, and n -propyl nitrites, have exhibited in their thermal decomposition the characteristics pertaining to homogeneous unimolecular reactions. This paper deals with the investigation carried out on iso -propyl nitrite decomposition. This member of the series is particularly interesting as it allows comparison to be made between a straight-chain and a branched-chain isomer. The effect of these chemical configurations on the activation energy and the decomposition rates can be very effectively studies as no complications enter into the reactions to confuse measurements. Experimental Reaction velocities were measured as before by observing the rate of pressure change in a system at constant volume. The reaction vessels were Pyrex glass bulbs with a capacity of about 125 cc. The apparatus was similar to that used in previous experiments. The connecting tubing was heated to 105° C to prevent any of the products of the reaction condensing out. Control and measurement of the temperature was carried out as before. The temperature could be maintained constant to within 0·25° C.

Biological activity of 2,4-D esters on rubber vine (Cryptostegia grandiflora): dependence on vapour pressure and molecular weight and isomerism of the alcohol substituent

1989 ◽  
Vol 40 (3) ◽  
pp. 685
Author(s):  
GJ Harvey
Keyword(s):  
Molecular Weight ◽  
Vapour Pressure ◽  
Low Molecular Weight ◽  
Straight Chain ◽  
Biological Efficacy ◽  
Cryptostegia Grandiflora ◽  
Normal Series ◽  
Branched Chain ◽  
The Relationship ◽  
Volatile Esters

The relationship between molecular structure and biological efficacy was investigated for 16 esters of 2,4-D [(2,4-dich1orophenoxy)acetic acid] on rubber vine (Cryptostegia grandiflora). These included the normal (n) or straight-chain esters from C-1 (methyl) to C-8 (octyl), the n-decyl, n-dodecyl, isobutyl, amyl (iso-pentyl), 2-ethylhexyl (iso-octyl), and the methoxy-, ethoxy-, and butoxyethyl esters. For the normal series esters, biological efficacy was found to be a function of both the molecular weight and the vapour pressure of the esters. This relationship was linear for the higher molecular weight, low volatile esters, biological efficacy decreasing with increasing molecular weight and the accompanying decrease in vapour pressure of the esters. The low molecular weight, volatile esters were more active than the higher molecular weight, low volatile esters, and increases in the vapour pressure of these low molecular weight, volatile esters were sufficient to account for the deviation from linearity of those esters. When all esters are considered, the same relationships hold but the branched-chain (iso) and chemically substituted (alkoxy alcohol) esters are less effective than the corresponding normal esters. Possible reasons for these results are discussed.

scholarly journals Synthesis, antimicrobial and anti-cancer activities of some new N-ethyl, N-benzyl and N-benzoyl-3-indolyl heterocycles

2012 ◽  
Vol 62 (2) ◽  
pp. 157-179 ◽  
Author(s):  
Eslam El-Sawy ◽  
Adel Mandour ◽  
Khaled Mahmoud ◽  
Inas Islam ◽  
Heba Abo-Salem
Keyword(s):  
Hydrazine Hydrate ◽  
Hydroxylamine Hydrochloride ◽  
Reference Drug ◽  
Highly Active ◽  
Anti Cancer ◽  
Hct 116 ◽  
New Compounds ◽  
Substituted 1 ◽  
Isoxazole Derivatives

Synthesis, antimicrobial and anti-cancer activities of some newN-ethyl,N-benzyl andN-benzoyl-3-indolyl heterocyclesA series of 1-(N-substituted-1H-indol-3-yl)-3-arylprop-2-ene-1-ones (2a, b-4a, b) were prepared and allowed to react with urea, thiourea or guanidine to give pyrimidine derivatives5a, b-13a, b. Reaction of2a, b-4a, bwith ethyl acetoacetate in the presence of a base gave cyclohexanone derivatives14a, b-16a, b. Reaction of the latter compounds with hydrazine hydrate afforded indazole derivatives17a, b-19a, b. On the other hand, reaction of2a, b-4a, bwith some hydrazine derivatives, namely hydrazine hydrate, acetyl hydrazine, phenylhydrazine and benzylhydrazine hydrochloride, led to the formation of pyrazole derivatives20a, b-31a, b. Moreover, reaction of2a, b-4a, bwith hydroxylamine hydrochloride gave isoxazole derivatives32a, b-34a, b. The newly synthesized compounds were tested for their antimicrobial activity and showed that 4-(N-ethyl-1H-indol-3-yl)-6-(p-chlorophenyl)-pyrimidine-2-amine (11b) was the most active of all the test compounds towardsCandida albicanscompared to the reference drug cycloheximide. Eighteen new compounds, namely pyrimidin-2(1H)-ones5a, b-7a, b, pyrimidin-2(1H)-thiones8a, b-10a, band pyrimidin-2-amines11a, b-13a, bderivatives, were tested for theirin vitroantiproliferative activity against HEPG2, MCF7 and HCT-116 cancer cell lines. 4-(N-ethyl-1H-indol-3-yl)-6-(p-methoxyphenyl)-pyrimidin-2-amine (11a)was found to be highly active withIC50of 0.7 μmol L-1.

Metabolic profiles in serum of mouse after chronic exposure to drinking water

2010 ◽  
Vol 30 (8) ◽  
pp. 1088-1095 ◽  
Author(s):  
Yan Zhang ◽  
Bing Wu ◽  
Xuxiang Zhang ◽  
Aimin Li ◽  
Shupei Cheng
Keyword(s):  
Drinking Water ◽  
Aromatic Hydrocarbons ◽  
Chronic Exposure ◽  
Metabolic Profiles ◽  
Clean Water ◽  
Branched Chain Amino Acid ◽  
Water Plant ◽  
Polycyclic Aromatic ◽  
Branched Chain ◽  
Total Concentrations

The toxicity of Nanjing drinking water on mouse (Mus musculus) was detected by 1H nuclear magnetic resonance (NMR)-based metabonomic method. Three groups of mice were fed with drinking water (produced by Nanjing BHK Water Plant), 3.8 μg/L benzo(a)pyrene as contrast, and clean water as control, respectively, for 90 days. It was observed that the levels of lactate, alanine, and creatinine in the mice fed with drinking water were increased and that of valine was decreased. The mice of drinking water group were successfully separated from control. The total concentrations of polycyclic aromatic hydrocarbons (PAHs), phthalates (PAEs), and other organic pollutants in the drinking water were 0.23 μg/L, 4.57 μg/L, and 0.34 μg/L, respectively. In this study, Nanjing drinking water was found to induce distinct perturbations of metabolic profiles on mouse including disorders of glucose-alanine cycle, branched-chain amino acid and energy metabolism, and dysfunction of kidney. This study suggests that metabonomic method is feasible and sensitive to evaluate potential toxic effects of drinking water.

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