- Antitumor imide derivatives of 7-oxabicyclo[2.2.1]heptane-2,3-dimethyl-2,3-dicarboxylic acid
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The imide and methylimide derivatives of 7-oxobicyclo-[2.2.1]heptane-2,3-dimethyl-2,3-dicarboxylic acid were synthesized and shown to have antitumor inhibitory activity (growth inhibition) against the KB cell line. The compounds were prepared according to standard procedures. Interest in the respective imide derivatives stemmed from their structural relationship to antitumor-active derivatives of 7-oxobicyclo[2.2.1]heptane-2,3-dicarboxylic acid which lacked 2,3-dimethyl substituents or which were derivatives of isoindolines and lacked the carbonyl groups.
- Walter
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- Cantharimide dimers from the Chinese blister beetle, Mylabris phalerate PALLAS
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Five cantharidin-related compounds were isolated from the Chinese blister beetle, Mylabris phalerate PALLAS (Meloidae). Their structures were determined based on spectroscopic and chemical evidence. Three of them were identified as cantharimide dimers, which consist of two units of cantharimide combined with a tri-, tetra-, or penta-methylene group.
- Nakatani, Takafumi,Jinpo, Katsuaki,Noda, Naoki
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- Synthesis of canthardin sulfanilamides and their acid anhydride analogues via a ring-opening reaction of activated aziridines and their associated pharmacological effects
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The cantharidinimide derivatives, 5a-h, including sulfanilamides containing pyrimidyl, pyrazinyl, hydrogen, thiazolyl, and oxazolyl groups were synthesized. Modification of cantharidinimide by means of the reaction of activated aziridine ring opening led to the discovery of a novel class of antitumor compounds. The analogues 10i-k, 11l-n, 12o-p, and 16q-s were obtained from treating cantharidinimide 6 and analogues (7, 8, and 13) with activated aziridines, which produced a series of ring-opened products including normal and abnormal types. Some of these compounds showed cytotoxic effects in vitro against HL-60, Hep3B, MCF7, and MDA-MB-231 cancer cells. The most potent cytostatic compound, N-cantharidinimido-sulfamethazine (5a), exhibited anti-HL-60 and anti-Hep3B cell activities. Two compounds 5g and 5h displayed slight effects on the Hep3B cell line, while the other compounds produced no response in these four cell lines.
- Chiang, Ling-Ling,Tseng, Ing-Jy,Lin, Pen-Yuan,Sheu, Shiow-Yunn,Lin, Ching-Tung,Hsieh, Yun-Han,Lin, Yi-Jing,Chen, Hsiao-Ling,Lin, Mei-Hsiang
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