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Biomedical subjects

F T Chiu

Publications and source records attributed to F T Chiu.

6 recordsLinked to original sources

Synthesis, hydrolytic reactivity, and anticancer evaluation of N- and O-triorganosilylated compounds as new types of potential prodrugs.

N- and O-Triorganosilylated compounds related to various anticancer agents were synthesized for evaluation as potential anticancer prodrugs. 1H-NMR and UV kinetic measurements of hydrolytic desilylation were used to correlate relative rates of structural unmasking with steric bulk about the silicon reaction center. The tert-butyldimethylsilyl ester of chlorambucil and a number of O- triorganosilylated carbamate derivatives of nor-nitrogen mustard showed significant activity against P-388 lymphocytic leukemia in mice.

Animals↗

Rifampicin associated renal dysfunction during antituberculous therapy.

Intermittent rifampicin therapy has been reported to commonly cause a flu-like illness with chills and fever sometimes associated with acute renal failure. This report describes a fourth case of partially reversible insidious renal damage associated with continuous rifampicin therapy and provides evidence that it is not the results of light chain proteinuria as previously suggested. A retrospective review of data relating to renal function in 89 tuberculous patients indicated that increased plasma urate concentration was commonly associated with ethambutol therapy.

Acute Kidney Injury↗

Synthesis, base-catalyzed hydrolytic reactivity, and anticancer evaluation of O-aryl phosphorodiamidates as a novel class of pro(phosphorodiamidic acid mustards).

Bis(2-chloroethyl)phosphoramidic dichloride [MP(O)Cl2, M = N(CH2CH2Cl)2] has been used as the starting material for the synthesis of O-aryl phosphorodiamidates having the general structure MP(O)(NHR)OAr: 9, R = H, Ar = 4-NO2C6H4; 10, R = H, Ar = C6F5; 11, R = C6H5, Ar = C6F5; 12, R = 4-MeC6H4, Ar = C6F5; and 13, R = 4-EtOC6H4, Ar = C6F5. The phosphorodiamidic chloride precursor to 13 (14) was also isolated. Kinetics for the base-catalyzed hydrolysis of compounds 9--13 were investigated by UV and NMR methods and are considered in connection with service of these compounds as pro(phosphorodiamidic acid mustards) [MP(O)(NHR)OAr leads to MP(O)(NHR)OH] via an E1cB mechanism involving the intermediacy of a mustard-bearing metaphosphorodiimide [MP(O)=NR]. Anticancer screening tests against L1210 lymphoid leukemia in mice indicated that 9--14 are inactive; similar negative results were obtained with the KB cell culture, except in the case of 14 which was marginally active.

Animals↗

Caviation in lung cancers.

This paper examines the incidence of cavitation among tumours of the lung, the various radiological appearances and cellular types of these cavitated tumours, and the resulted of sputum cytology. Over a 46 months' period, histological and or cytological evidence of pulmonary neoplasm was found in 244 subjects whose posteroanterior chest radiographs showed opacities suggestive of pulmonary malignant disease. Of the 244 lung tumours, 220 (90%) were primary and 24 (10%) were secondary. Twenty-seven tumours (11%) were cavitated. Every cavitated tumour but one was a primary lung neoplasm. Twenty-one (81%) of these 26 cavitated primary lung tumours were squamous cell carcinoma. Large cell undifferentiated carcinoma (two cases of 7%), adenocarcinoma (one case or 4%) small cell undifferentiated carcinoma (one case or 4%) and alveolar cell carcinoma (one case or 4%) made up the rest. Sputum was examined for cells on 185 patients with primary solid and in 25 patients with primary cavitated lung cancers. Cancer cells were found in 152 patients (72%). Surprisingly, the finding of cancer cells in the sputum was no more frequent in cavitated tumours than in solid tumours. It is concluded that if a cavitated lesion in the radiograph is maglinant, a primary squamous cell carcinoma of the lung is the most likely cause. Sputum cytology performed by a competent cytologist is a very useful and simple diagnostic tool, but it appears to be no more helpful in diagnosing cavitated than in solid lung cancers.

Adenocarcinoma↗