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Biomedical subjects

C C Cheng

Publications and source records attributed to C C Cheng.

At least 145 records · Page 8Linked to original sources

Difference in antimalarial activity between certain amino alcohol diastereomers.

A striking difference in antimalarial activity between the diastereomers of 6-bromo-alpha-[2-(1-methylpiperidyl)]-9-phenanthrenemethanol, alpha-(3-peperidyl)-3,6-bis(trifluoromethyl)-9-phenanthrenemethanol, and alpha-(3-piperidyl)-2,8-bis(trifluoromethyl)-4-quinolinemethanol was observed. A possible explanation involving the N-O distance and active site binding requirements is suggested.

Amino Alcohols↗

Some substituted naphthazarins as potential anticancer agents.

Some 2,3-bis(substituted methyl)naphthazarins and related compounds were synthesized by the Diels-Alder reaction of benzoquinone and 2,3-dimethylbutadiene followed by oxidation and substitution reactions. These compounds were prepared as potential biological alkylating agents. Screening results indicated that 1,4-diacetyl-6,7-dimethyl-4a,5,8,8a-tetrahydronaphthalene and 5,8-bis(benzoyloxy)-2,3-dimethyl-1,4-naphthoquinone possessed borderline activity against leukemia P388 and that naphthazarin diacetate possessed confirmed cytotoxicity against the cell culture of human epidermoid carcinoma of the nasopharynx.

Animals↗

Tetramethoxydibenzoquinolizinium salts. Preparation and antileukemic activity of some positional and structural isomers of coralyne.

Some positional and structural isomers of coralyne were prepared and evaluated in the P388 lymphocytic leukemia system for their inhibitory activity. The levels of antileukemic activity of coralyne, neocoralyne, isocoralyne, and stracoralyne were comparable, thus implying that two sets of the N-O-O triangular pharmacophore in a condensed isoquinoline molecule are preferable and the angle between these two sets has little influence on antileukemic activity. The importance of the environment around the C5-C6 region of the dibenzo[a,g]quinolizine ring to antileukemic activity was demonstrated by the activity differences between coralyne and allocoralyne.

Animals↗

Solubilization and stabilization of the cytotoxic agent coralyne.

Kinetic studies were carried out on the ring opening of the quaternary nitrogen cation, coralynium ion (I), to yield 6'-acetylpapaverine (III), on the cyclization of III to yield I, and on a photochemical reaction undergone by I in aqueous solutions exposed to visible light. From the results, it was concluded that: (a) I and III are in facile equilibrium in aqueous solution but appreciable amounts of III do not exist in dilute solutions with pH values below 10: (b) the photochemical reaction of I in water (presumably a photohydration) can be reversed by lyophilization, by heatiing, and by increasing the pH of solutions to values greater than 12; (c) the photochemical reaction of I can be inhibited by protecting the aqueous solutions from visible light, and the rate in the presence of light can be reduced by increasing the concentration of I in the solution; and (d) although the chloride and sulfoacetate salts of I react identically and have similar solubilities in water, it is possible to prepare more concentrated and, hence, more stable solutions of the sulfoacetate salt by including sodium hydroxide in the solvent. The solubility of coralyne chloride remains about the same in dilute sodium hydroxide as in water.

Antineoplastic Agents↗

Preparation and antileukemic activity of some alkoxybenzo(c)phenanthridinium salts and corresponding dihydro derivatives.

Salts of 2,3,8,9-tetrasubstituted alkoxy-, hydroxy-, and acetoxybenzo(c)phenanthridines as well as the corresponding 6-methoxy-5,6-dihydrobenzo(c)phenanthridines were prepared from appropriate chalcones through the tetralone and the 4b,10b,11,12-tetrahydrobenzo(c)phenanthridine intermediates. Complete O-demethylation of the tetramethoxybenzophenanthridine was achieved by fusion with pyridine hydrochloride at elevated temperature. The title compounds are active against leukemias L1210 and P388 in mice and some are curative against Lewis lung carcinoma. The importance of the nature of the environment about the nitrogen atom of these compounds and the substituents is discussed. 3,4-Dimethoxy-3,4-methylenedioxychalcone possesses activity against leukemia P388.

Animals↗

4-Hydroxyurazole.

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Azaguanine↗