Cytostatic Activity of Combretastatin A-4 Derivatives in an In Vitro System.

Cytostatic activity of combretastatin A-4, its 11 analogues, and paclitaxel (Taxacad) was evaluated in vitro on human tumor cells A549 (lung adenocarcinoma) and PC-3 (prostate adenocarcinoma) in order to find the active and stable compound as a promising antitumor agent. 5-(4-Methoxyphenyl)-4-(3,4,5-trimethoxyphenyl)-isoxazole (compound 123124) and 3-(3,4,5-trimethoxyphenyl)-4-(4-methoxyphenyl)-isoxazole (compound 29310186) demonstrated the highest cytostatic activity (IC≈8×10 М). The activity of two other cytotoxic compounds (2E)-1-(7-methoxy-2H-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one (compound 104815) and 4-(3-amino-4-methoxyphenyl)-5-(3,4,5-trimethoxyphenyl)-1H-pyrazole hydrochloride (compound 198732) was close to that of Taxacad: IC 65×10 and 80×10 М, respectively, and are also promising active components for the development of antitumor drugs.

Electrochemically Induced Synthesis of Sulfonylated -Unsubstituted Enamines from Vinyl Azides and Sulfonyl Hydrazides.

Sulfonylated -unsubstituted enamines were synthesized through a chain of chemical and electrochemical transformations via sulfonylation of vinyl azides. The disclosing of the -unsubstituted enamines synthesis was based on a unique property of the azido group, which is its ability to eliminate the N molecule. Furthermore, a formal paradox is observed: a double bond reacts and a double bond is retained.

Synthesis and structure of 2,4,6-tri-cyclo-butyl-1,3,5-trioxane.

The synthesis and structure of 2,4,6,-tri-cyclo-butyl-1,3,5-trioxane, CHO , is described. It was formed in 39% yield during the work-up of the Swern oxidation of cyclo-butyl-methanol and may serve as a stable precursor of the cyclo-butane carbaldehyde. The mol-ecule of occupies a special position (3.

Sea Urchin Embryo Model As a Reliable in Vivo Phenotypic Screen to Characterize Selective Antimitotic Molecules. Comparative evaluation of Combretapyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles as Tubulin-Binding Agents.

A series of both novel and reported combretastatin analogues, including diarylpyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles, were synthesized via improved protocols to evaluate their antimitotic antitubulin activity using in vivo sea urchin embryo assay and a panel of human cancer cells. A systematic comparative structure-activity relationship studies of these compounds were conducted. Pyrazoles 1i and 1p, isoxazole 3a, and triazole 7b were found to be the most potent antimitotics across all tested compounds causing cleavage alteration of the sea urchin embryo at 1, 0.

Rearrangements of organic peroxides and related processes.

This review is the first to collate and summarize main data on named and unnamed rearrangement reactions of peroxides. It should be noted, that in the chemistry of peroxides two types of processes are considered under the term rearrangements. These are conventional rearrangements occurring with the retention of the molecular weight and transformations of one of the peroxide moieties after O-O-bond cleavage.