Abstract

A convenient method for the synthesis of new series of N-acylsulfamoyl-oxazolidin-2-one containing nitrogen mustard moiety starting from chlorosulfonyl isocyanate, chiral oxazolidinone and nitrogen mustard in two steps (carbamoylation, sulfamoylation) is described herein. The synthesis of these compounds has been carried out in good isolated yields (71–89%). The structures of all synthesized compounds were unambiguously confirmed by usual spectroscopic methods 1H NMR, 13C NMR, IR, EA and MS. The molecular structure of 3c was obtained by X-ray diffraction on mono crystal. The newly synthesized products were evaluated for their in vitro antitumor activity against different human cancer cell lines (PRI, K562 and JURKAT). A computational analyses Petra/Osiris/Molinspiration (POM) has been developed with the aim of evaluating the performance of physico-chemical properties of tested compounds, and to get insights on the degree of their toxicity.

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