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Results for “Cyclohexanones”

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At least 127 records · Page 7Linked to original sources
PubMed2002

Analysis of rat bone marrow by flow cytometry following in vivo exposure to cyclohexanone oxime or daunomycin HCl.

The purpose of these studies was to evaluate bone marrow from male CD rats following exposure to known hematotoxins using flow cytometry (FC) and a monoclonal antibody to the cell surface antigen CD71. Rats were treated with either CHO (300 mg/kg for 10 days) or DAUN (10 mg/kg for 1 day). Control groups received the appropriate vehicle. Half of the animals from each group were euthanized at the end of the dosing schedule and the remaining animals were euthanized after a recovery period. Hematology analyses were completed prior to the onset of each study and on the day of necropsy. Marrow was isolated from the tibia, stained with R-phycoerythrin-conjugated mouse anti-rat CD71 (transferrin receptor on proliferating cells) monoclonal antibody, and then analyzed by FC for myeloid:erythroid (M:E) ratios. FC determinations of myeloid and erythroid population percentages and M:E ratios from untreated rats were confirmed by microscopic examination of marrow cytospins and selected flow cell sorts. M:E ratios for control animals determined by FC were not significantly different between the two studies (1.83 vs 1.89). CHO treatment caused a significant (p < 0.01) decrease in M:E ratios (0.96 for CHO vs 1.48 for control) at day 11 due to increased erythroid cells. M:E ratios were significantly increased (p < 0.05) with DAUN treatment at day 3 (5.07 for DAUN vs 1.70 for control) and corresponded to generalized depletion of all marrow cell lines, especially erythroid cells. After recovery, M:E ratios of CHO and DAUN rats were similar to controls. Hematological values corroborated changes in marrow myeloid and erythroid populations evaluated by this FC technique. Using FC and a monoclonal antibody to the cell surface antigen CD71, this study confirmed the reversible selective toxicity on myeloid and erythroid marrow populations following in vivo exposure to CHO or DAUN. This FC procedure provides a rapid, sensitive method for bone marrow analysis compared to conventional cytological examination.

Animals↗
PubMed2004

2,6-Bis(3,4,5-trihydroxybenzylydene) derivatives of cyclohexanone: novel potent HIV-1 integrase inhibitors that prevent HIV-1 multiplication in cell-based assays.

A number of 2,6-bisbenzylidenecyclohexane-1-one derivatives have been synthesized and tested as HIV-1 integrase (IN) inhibitors with the aim of obtaining compounds capable to elicit antiviral activity at non-cytotoxic concentrations in cell-based assays. 3,5-Bis(3,4,5-trihydroxybenzylidene)-4-oxocyclohexaneacetic acid (20d) resulted one of the most potent and selective derivatives in acutely infected MT-4 cells (EC(50) and CC(50) values of 2 and 40 microM, respectively). In enzyme assays with recombinant HIV-1 integrase (rIN), this compound proved able to inhibit both 3'-processing and disintegration with IC(50) values of 0.2 and 0.5 microM, respectively. In order to develop a model capable to predict the anti HIV-IN activity and useful to design novel derivatives, we performed a comparative molecular field analysis (CoMFA) like 3-D-QSAR. In our model the ligands were described quantitatively in the GRID program, and the model was optimized by selecting only the most informative variables in the GOLPE program. We found the predictive ability of the model to increase significantly when the number of variables was reduced from 20,925 to 1327. A Q(2) of 0.73 was obtained with the final model, confirming the predictive ability of the model. By studying the PLS coefficients in informative 3-D contour plots, ideas for the synthesis of new compounds could be generated.

Anti-HIV Agents↗
PubMed2003

Cytotoxic analogues of 2,6-bis(arylidene)cyclohexanones.

A series of 2,6-bis(arylidene)cycloalkanones (1) and related compounds containing one or two substituents at the four position of the cyclohexyl ring were prepared and shown to display cytotoxic activity towards murine P388 and L1210 cells as well as human Molt 4/C8 and CEM T-lymphocytes. In some of the series of compounds, positive correlations were noted between the potencies of the enones and the magnitude of the Hammett sigma values of the aryl substituents. Four representative compounds were cytotoxic to a number of human tumours in vitro, particularly towards colon cancer and leukemic cells. A noteworthy feature of the compounds prepared in this study is that, in general, they were well tolerated when administered to rodents. A number of lead molecules emerged from this investigation as well as guidelines for future expansion of these series of compounds.

Animals↗
PubMedDate not supplied

A base-catalyzed solution-phase parallel synthesis of substituted vinylic benzamides from 3-amino-2-cyclohexanones.

An improved method for the synthesis of benzamides from 3-amino-2-cyclohexenones is presented. Using sodium hydride, a base-catalyzed N-benzoylation provided significantly higher yields (71-79%) for the reported compounds. This novel protocol was applied in the solution-phase parallel synthesis of a 12-member library of vinylic benzamide derivatives of 3-amino-2-cyclohexenones in 63-90% yield, using a Radley's Carousel Reaction Station.

Benzamides↗