Organophosphorus compounds have been investigated for applications in agricultural and medicinal applications for decades, and a considerable number of phosphorus-containing drugs have achieved commercial success. Recently by P. Finkbeiner atc in review have shown, that phosphine oxides and related phosphorus-containing functional groups are valuable polar structural elements and that they deserve to be considered as a routine part of every medicinal chemist’s toolbox. A new approach to the synthesis of previously hard-to-obtained 3-alkyl-1H-phospholanes oxides was developed by us. In order to assess the potential of five-membered cyclic organophosphorus compounds in cancer therapy, we carried out docking 3-buthyl-1H-phospholanes oxide and 2,3-dihydrophosphole in the binding site of 24 human proteins involved in oncogenesis processes. Proteins were selected using the PharmMapper in-house pharmacophore model database. The results are presented in the article.