New di-(β-chloroethyl)-α-amides on N-(meta-Acylaminobenzoyl)-D, L-aminoacid supports with antitumoral activity

cited By 8International audienceIn order to obtain new compounds with antitumoural action the N-(meta-acylaminobenzoyl)-α-acylaminobenzoyl)-α-aminoacids 4-9 were prepared. These compounds were subsequently converted into the corresponding Δ2-oxazolin-5-ones 10-15, which in turn were submitted to a ring opening reaction with di-(β-chloroethyl)amine to afford the peptide supported N-mustards 16-21, which showed low toxicity and cytostatic activity similar to that of sarcolisine against the Ehrlich ascite and Walker 253 carcinosarcoma. © 2007 by MDPI

Synthesis and biological activity of some new 1,3,4-thiadiazole and 1,2,4-triazole compounds containing a phenylalanine moiety

cited By 48International audienceNew 1,3,4-thiadiazole, 6, 7 and 1,2,4-triazole derivatives, 8, 9 containing a phenylalanine moiety have been synthesized by intramolecular cyclization of 1,4- disubstituted thiosemicarbazides, 4, 5, in acid and alkaline media, respectively; the thiosemicarbazides were obtained by reaction of hydrazide 3 with appropriate aromatic isothiocyanates. The toxicity of the synthesized compounds was evaluated and the antiinflammatory study of the triazole compound 9 established an appreciable antiinflammatory activity that is comparable with that of other nonsteroidal anti-inflammatory agents. © 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland

THE ANTIOXIDANT POTENTIAL EVALUATION OF DICLOFENAC DERIVATIVES WITH HYDRAZONES STRUCTURE

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