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At least 127 records · Page 7Linked to original sources
PubMed1987

Synthesis and antitumor activity of tropolone derivatives. 4.

Modifications of monotropolone 2 having poor potency against P388 in mice were studied. The alpha-ethoxy group of 2, prepared from hinokitiol and benzaldehyde diethyl acetal, was replaced with a phenolic or heteroaromatic compound by heating 2 with the appropriate nucleophile. Structure-activity relationships indicated that an acidic hydroxyl and a proton-accepting group situated in the neighboring position, which permits the formation of a chelate with a metal ion, contributed to enhanced activity. Among the compounds studied, the 8-hydroxyquinoline analogue 10f was the most favorable compound.

Animals↗
PubMed1992

Imbalance of deoxyribonucleoside triphosphates and DNA double-strand breaks in mouse mammary tumor FM3A cells treated in vitro with an antineoplastic tropolone derivative.

The mechanism by which alpha,alpha-bis(2-hydroxy-6-isopropyltropon-3-yl)-4-methoxytolu ene (JCI-3661) kills mouse mammary tumor FM3A (F28-7) cells was studied. When the cells were exposed to the drug at 3.7 microM, the intracellular dNTP pool became imbalanced because of decreases in dGTP and dATP and an increase in dTTP. The pattern of the dNTP imbalance was the same as that caused by hydroxyurea. When JCI-3661 was added to the culture medium, mature DNA strands broke, giving fragments of 100-200 kilobase pairs long as found by orthogonal-field-alternation gel electrophoresis. DNA strand breaks, detected by this technique, were observed in the cells at 12 h after the addition. The beginning of cell death was observed at about 14 h (trypan blue staining) or at about 12 h (colony-forming ability) after cultivation Breaks in the single and double strands of DNA, as measured by alkaline and neutral filter elution assay, became evident 24 h after treatment with 3.7 microM JCI-3661. Comparison of the ratio of single- and double-strand breaks caused by JCI-3661 to that following radiation suggested that JCI-3661 broke only double strands. Cycloheximide inhibited both the breakage of double strands and the cell death caused by JCI-3661. JCI-3661 decreased DNA synthesis more than RNA or protein synthesis. The breaks in double strands of DNA were probably important in the cell death caused by JCI-3661.

Animals↗
PubMed1991

A new dual-label technique for platelet survival studies with the use of 111indium and 114mindium tropolonate.

A dual-label technique to study the survival of two different populations of platelets within one individual was developed using 111indium and 114mindium. The validity of the technique was demonstrated in seven individuals with an expected equal survival time of two platelet populations and in two persons with an expected difference in platelet survival time. Since the energy spectra of the two indium isotopes are very close, a well-type germanium semiconductor detector was applied. By adaptation of the counting time the effective dose equivalent of the dual-label procedure could be restricted to 1.6 mSv. The dual-label technique provides an instrument for studying the survival of two different populations of platelets simultaneously within one individual.

Adult↗