A series of 2-anilinopyrimidines was prepared and their fungicidal activities against Botrytis cinerea Pers were examined. The activity fell sharply with any substitution on the anilinobenzene ring. Substituents at the 5-position of the pyrimidine ring greatly reduced the activity. Substituents such as chloro, methoxy, methylamino, methyl or 1-propynyl were well tolerated at the 4- and 6-positions of the pyrimidine ring. Among these substituents, the combination of methyl and 1-propynyl groups was the most favourable. 2-Anilino-4-methyl-6-(1-propynyl)pyrimidine (KIF-3535), which showed excellent activity and no significant phytotoxicity, was finally selected for development and has been given the common name mepanipyrim.

The degree of the optic nerve kinking angle was an independent predictor of postoperative improvement, indicating that irreversible damage to the optic nerve may be associated with its kinking at the optic canal orifice.

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Mepanipyrim, N-(4-methyl-6-prop-l-ynylpyrimidin-2-yl)aniline, hardly inhibited the mycelial respiration and the syntheses of DNA, RNA, protein, lipids and cell walls in mycelia of Botrytis cineyea at 100 eg/ml. By the treatment of mepanipyrim at 10-100 g/ml, each uptake of 14C-labeled glucose, acetate, uridine, thymidine, alanine or glucosamine by the mycelia of B. cineyea was inhibited, but no apparent uptake inhibition of these precursors was observed below 1, csg/ml. The inhibition by mepanipyrim of the active transport process across the cellular membrane may bring about a chronic deficiency in most intracellular substrates essential for growth and development. However, the effect of mepanipyrim appeared not to be strong enough to disrupt the overall functions of cell membrane in B. cineyea; because it neither stimulated the leakage of protein, phosphate, glucose and electrolytes from the cells, nor influenced the bursting rate of protoplasts by osmotic shock.

Markedly inhibitory effects of Ca2؉ ؉ on the growth of human tumor cells were attained through the induction of apoptosis in vitro. On the other hand, a good correlation between the growth inhibition effects of Ca 2؉ ؉ and the amounts of phosphatidylserines (PS) in the cell membranes (plasma membranes) was obtained. Furthermore, the decrease of membrane fluidity and the localization of lipid microdomains "lipid rafts" in the cell membranes were observed in the presence of Ca 2؉ ؉ . The findings in this study suggest that Ca 2؉ ؉ could induce apoptosis toward tumor cells through the localization of lipid rafts in plasma membranes by the specific interactions between extracellular Ca 2؉ ؉ and PS.

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