- Novel benzopyridothiadiazepines as potential active antitumor agents
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The synthesis of novel thiadiazepine derivatives, that could be considered as constraint analogues of E-7010, are reported. These molecules were evaluated for their antiproliferative activity toward the murine L1210 leukemia cell line. Flow cytometric studies performed on L1210 cells with the most cytotoxic compounds showed an accumulation of the cells in the G2/M phases of the cell cycle with a significant percentage of tetraploid cells (8N DNA content). Submicromolar cytotoxicities were observed with compounds 2b, 4b, 4e, 4g, and 4i. Two of them, compounds 2b and 4b, were found to be potent inhibitors of tubulin polymerization with IC50 of respectively 3.8 and 2.4 μM compared to 2.4 μM for desoxypodophyllotoxin. A 4-methoxyphenylethyl substitution on the pyridinyl nitrogen of the benzopyridothiadiazepine was found to be essential for the antiproliferative activity. The in vitro activities of compounds 2b and 4b make benzopyridothiadiazepine dioxides a promising new class of tubulin binders which warrant further in vivo evaluation.
- Lebegue, Nicolas,Gallet, Sebastien,Flouquet, Nathalie,Carato, Pascal,Pfeiffer, Bruno,Renard, Pierre,Léonce, Stéphane,Pierré, Alain,Chavatte, Philippe,Berthelot, Pascal
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p. 7363 - 7373
(2007/10/03)
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- Sulfonamides as antifungal agents
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The present invention relates to new sulfonamides having the formula I: STR1 wherein: R1 represents an alkyl, aryl or heteroaryl group; R2 is hydrogen or an alkyl, aryl or heteroaryl group; or R1 and R2 may form a ring; R3 is hydrogen or may form an oxazolidine ring together with R2, and this ring may be optionally substituted by one or two alkyl, aryl or heteroaryl groups at the postion 2; R7 is hydrogen or alkyl; X is CH or N; Ar is a phenyl ring or a substituted phenyl ring. The invention also relates to a procedure for their preparation and to pharmaceutical and agrochemical compositions containing them. These compounds are antifungal agents.
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