• Archives of Pharmacal Research
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• v.25 no.6
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• pp.781-785
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• 2002

A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.

• Archives of Pharmacal Research
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• v.23 no.2
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• pp.99-103
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• 2000

Acid and base catalyzed intramolecular cyclizations of N-benzoylthioureidoacetal, contain-ing four functional groups adjacent to thiourea such as benzocarbamoyl, acetal, thioure and amide, were investigated. The condensation reaction of N-benzoyl thiocarbamoylgly-cine amide in the presence of 10% aqueous NaOH provided 1-(2,2-dimethoxy)ethyl-imi- dazolidine-2-thione exclusively. In the presence of pyridine, it was transformed to 2- thiohydantoin. N-Benzoyl thiocarbamoyl glycine amide was completely transformed to an iminothiazolidine exclusively in the presence of Lewis acid such as borontrifluoride ether-ate or trimethylsilyl iodide. 1-(2,2-Dimethoxy)ethyl-imidazolidine-2-thione was transformed to imidazole[2,1-b]thiazole and pyrazino[5,1-a]imidazole in the presence of $BF_3$.$ET_2$O and formic acid, respectively.

• The Korean Journal of Pesticide Science
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• v.9 no.2
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• pp.153-158
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• 2005

Safening activities of optically active ${\alpha}$-methylbenzylphenylureas on crop injury of rice (Oryza sativa L., cv. Tsukinohikari, japonica) caused by bensulfuron-methyl (methyl 2-[[[[[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl]amino]sulfonyl]methyl]benzoate) and pyribenzoxim (benzophenone o-[2,6-bis[(4,6-dimethoxy-2-pyrimidinyl)oxy]benzoyl]oxime) were investigated. Some derivatives of the optically active compounds exhibited strong safening activity against growth inhibition of rice by bensulfuron-methyl. Out of the derivatives tested, (S)-2,3-diCl and (S)-2-F-4-Me derivatives showed greater relieving activity than that of dymuron. In addition, the stress relieving activity was also obtained when they were applied at 4 days after bensulfuron-methyl treatment. On the other hand, crop injury caused by pyribenzoxim was relieved by about 95% with (S)-2-F-4-Me derivative in shoots and roots of rice seedlings.