A library of novel 2-(het)arylpyrrolidine-1-carboxamides were obtained via a modular approach based on the intramolecular cyclization/Mannich-type reaction of N-(4,4-diethoxybutyl)ureas. Their anti-cancer activities both in vitro and in vivo were tested. The in vitro activity of some compounds towards M-Hela tumor cell lines was twice that of the reference drug tamoxifen, whereas cytotoxicity towards normal Chang liver cell did not exceed the tamoxifen toxicity. In vivo studies showed that the number of surviving animals on day 60 of observation was up to 83% and increased life span (ILS) was up to 447%. Additionally, some pyrrolidine-1-carboxamides possessing a benzofuroxan moiety obtained were found to effectively suppress bacterial biofilm growth. Thus, these compounds are promising candidates for further development both as anti-cancer and anti-bacterial agents.

The crystal and molecular structure of 1,1c-dimethyl-isoindigo is studied by single crystal X-ray diffraction analysis. It is shown that the molecules of 1,1c-dimethyl-isoindigo are nonplanar due to the rotation of two oxindole rings relative to the double bond. Keywords: single crystal X-ray diffraction analysis, isoindigo, conformation of molecules, intermolecular interactions.Isoindigo [1H,1cH-bis(indoline-3-ylidene)-2,2c-dion] and especially its derivatives containing an alkyl or arylmethyl substituent at the nitrogen atom have recently attracted close attention of the researchers, primarily because these compounds exhibit a wide range of biological activities [1][2][3][4]. Thus, N-methylisoindigo, patented as Meisoindigo, is a therapeutic agent in the treatment of chronic myelogenic leukemia [5]. However, the study of these compounds mostly deals only with their chemical and biochemical properties, whereas the structural issues have been given limited attention [6,7]. However, it is important to understand the structural features of the molecules of isoindigo derivatives to determine their bonding with specific bioligands.Experimental. The synthesis of 1,1c-dimethyl-isoindigo is described in [12]. The crystals are obtained by recrystallization from chloroform.The single crystal X-ray diffraction study was performed on a Smart Apex II CCD (OMoK D ) diffractometer at the Division of X-ray Diffraction Studies of the Spectral Analytical Center of the Russian Foundation for Basic Research. The structure was solved by a direct method using the SIR software [13] and refined first in the isotropic and then in the anisotropic approximation using the SHELXL-97 software [14]. The sites of hydrogen atoms were found from the difference series of electron density; their refinement was isotropic. All calculations were carried out using the WinGX [15] and APEX2

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Imidazolidin-2-one and 1,3-benzodiazepin-2-one scaffolds are structural motifs of many biologically active compounds. Herein, we report a highly regioselective acid-catalyzed intramolecular nucleophilic cyclization/intermolecular electrophilic substitution reaction sequence of (2,2-dialkoxyethyl)ureas. The reaction benefits from readily available starting materials, a simple workup procedure, moderate to high yields of target compounds, and provides a convenient entry to previously unknown 4-(het)arylimidazolidinones and 5-(het)arylbenzodiazepinones. The proposed mechanism of the reaction is also discussed.