A new family of potential oncostatics: 2-Chloroethylnitrososulfamides (CENS) - I. Synthesis, structure, and pharmacological evaluation (preliminary results)

Article abstract of DOI:10.1016/0968-0896(96)00118-6

A new series of alkylating agents, 2-chloroethylnitrososulfamides (CENS), were developed on the model of 2-chloroethylnitrosoureas. Starting from chlorosulfonyl isocyanate, a four-step synthesis (carbamoylation-sulfamoylation, Mitsunobu alkylation, deprotection, and nitrosation) gives the title compounds in a 47-58% overall yield. The selection of the nitrosation site can be directed through an alternative route. The pharmacological evaluation shows a significant oncostatic activity towards both A549 and MCF7 cell lines.