Several fused tri- and tetracyclic quinolines (I and II) with [2-methoxy-4-[(methylsulfonyl)amino]phenyl]amino or [3-(N,N-dimethylamino)propyl]amino side chains were prepared, and their DNA intercalative properties, KB cytotoxicity, antitumor activity (P388 leukemia), and ability to induce topoisomerase II dependent DNA cleavage were investigated. Some compounds having both intercalative ability and KB cytotoxicity were found to be inactive in vivo. However, a positive correlation was seen between the ability to induce topoisomerase II dependent DNA cleavage and antitumor activity in vivo. The indeno- (13a), benzofuro- (21a), and benzothieno- (22a) quinoline derivatives exhibited potent antitumor activities in vitro and in vivo, comparable to those of m-AMSA. They also intercalate DNA and induce topoisomerase II dependent DNA cleavage. Extended screening of 13a showed it to be active against solid tumors such as M5076 sarcoma, B16 melanoma, and colon 38 carcinoma.

C6H9FN203, M.W. 176.15, tetragonal, I4~/a, a=b=21.102 (3), c=7.141 (1) A, Dm=l'49, Dx= 1.47 g cm -3, Z= 16. The final R was 0.042 for 1298 reflexions [I> 3~r(l)]. The configuration of the product from the addition of methyl hypofluoride to the C(5)= C(6) bond of 1-methyluracil is cis.

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To evaluate the usefulness of the screening test of the two-step bed side examination of swallowing function, we retrospectively analyzed 145 patients who were admitted to Nagoya Memorial Hospital with aspiration pneumonia between April 2015 and March 2016. The screening of swallowing function was performed by a multidisciplinary team in October, 2015. Then, the duration of hospital stay along with the patients＇ characteristics, such as age, sex, and underlying diseases, the severity of pneumonia defined by the A-DROP system, laboratory data (white blood cell count, C-reactive protein level, and albumin level), results of sputum bacterial cultures, and antibiotic therapy, were compared in patients between before (group A, n = 65) and after introducing the screening test of swallowing function (group B, n = 80). Aspiration risks were categorized into 4 grades using a standard sequential screening system; high, moderate, low, and none. Initiation of the screening test of swallowing function significantly reduced the number of inpatients whose duration of stay was more than 3 weeks (group A, 45/ 65 [69.2％] versus group B, 42/ 80 [52.5％]; P < 0.05, Fisher＇s exact test). This finding can mainly be attributed to the proper assessment of the aspiration risk, which enabled determination of the food form and the time to start oral ingestion without any incidents or accidents, and can facilitate the rapid intervention by a speech therapist and expert nurse.

ChemInform Abstract Chlorination of the tricyclic ketones (I) followed by coupling with the amine (II) gives the fused quinoline derivatives (III) with an amino side chain. The sulfur analogue (VIII) is prepared from anthranilic acid (IV) as outlined in the reaction scheme. Some of the fused tetracyclic quinoline derivatives (IX), which are prepared by similar procedures, show potent antitumor activities in vitro and in vivo.