Utility of thiophene-2-carbonyl isothiocyanate as a precursor for the synthesis of 1,2,4-triazole, 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives with evaluation of their antitumor and antimicrobial activities

<p>The reaction of thiophene-2-carbonyl isothiocyanate with phenylhydrazine gave 1-phenyl-5-(thien-2-yl)-1,2,4-triazole-3-thiol which was transformed by follow-up reactions into derivatives substituted in the 3-position by 1,2,4-oxadiazole and 1,2,4-thiadiazole moieties via thioethers linkages. The antitumor activity of the products against two human tumor cell lines, namely hepatocellular carcinoma HePG-2 and mammary gland breast cancer MCF-7 as well as the antimicrobial activity of some of these compounds was evaluated.</p

Dodecanoyl thiosemicarbazide derivatives as useful synthons in the synthesis of 1,2,4-triazole, 1,3,4-thiadiazole, and 1,3-benzothiazole derivatives

<p>A convenient synthesis of the dodecanoyl thiosemicarbazide derivatives <b>3a, b</b> has been achieved from the reaction of 2-benzamido-3-arylacryloylhydrazides <b>1a, b</b> and lauroyl isothiocyanate <b>(2)</b>. The thiosemicarbazide derivative <b>3a</b> is used as precursor for synthesis of 1,2,4-triazole, 1,3,4-thiadiazole, and 1,3-benzothiazole derivatives. The antimicrobial activity of some of the synthesized compounds was tested.</p

Synthesis and antitumor activity evaluation of some novel pyrazolotriazine derivatives

<p>6-Aminopyrazolo[1,2-<i>a</i>][1,2,4]triazine-4,8-dione derivative <b>3</b> was obtained upon the reaction of the acid hydrazide derivative <b>2a</b> with ethyl cyanoacetate. The reactions of <b>3</b> with several electrophiles such as aldehydes, isatin, acetic anhydride, phenyl isocyanate, benzoyl isothiocyanate, and <i>p</i>-toluenesulfonyl chloride were studied. The structures of the newly synthesized compounds were established on the basis of IR, ¹H NMR, mass spectra, and elemental analyses. The antitumor activities of some selective compounds were examined against two cell lines as liver carcinoma cell line (HEPG-2) and human breast cancer cell line (MCF7).</p