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Thermal ellipsoid representation of compound 3a.

Herein, we describe the synthesis of acyl azides and acyl urea glycals, a new class of C‐2 branched glycoconjugates, employing Pd‐catalyzed carbonylative coupling. A new strategy was developed to obtain acyl azides by carbonylative coupling between 2‐iodo‐glycals and NaN3 catalyzed by Pd(dba)2/Xantphos and carbon monoxide as a carbonyl source. Acyl azide glycals were used as synthetic intermediates in obtaining new acyl urea glycals via carbonylative coupling catalyzed by Pd(OAc)2 and 1,10‐Phen. Different glycal substrates, including disaccharide‐type, were studied, and various acyl azides and acyl ureas were prepared. Reaction yields were moderate to high (31–99 %) and reaction time varying from short to long (0.5–20 h).

Among poly(ADP-ribose) polymerases (PARPs), PARP-1 has emerged as a target in cancer therapy. The present work was aimed to design and synthesize O-alkylaryl amidoximes as a new antiproliferative agents. The target compounds were designed through the study of molecular docking against the PARP-1 and synthesized from commercially available starting materials in good yields under mild conditions and easy to perform reactions. The synthesized compounds exhibited in vitro antineoplastic activity (0.32-27.8 mM) against MCF-7 and Caco-2 cells, and one of them exhibited selective toxicity when tested against VERO cells. These compounds can be considered good candidates for the next stages in the development of new antiproliferative drugs.