Synthesis, characterization and biological investigation of steroid derivatives and their molecular aggregates

Our research proposal includes chemical transformations of some naturally occurring steroidal compounds and synthesis of new modified steroids in androstane and estra-1,3,5(10)-triene series. These newly synthesized compounds contain structural features present in the known and potent anticancer agents. We are also planning QSAR studies that would correlate and compare the structures with the biological activity of newly synthesized steroidal derivatives. Biological activity of the newly synthesized compounds will be tested, firstly on antitumor activity, and then on genotoxicity (for compounds showing evidence of antitumor potential). Furthermore, derivations of bile acids in order to get new steroidal surfactants are planed, as well as testing of their aggregation ability and membranotoxicity. Promoter activity of new steroidal compounds in the transport of selected drugs is also planed to be tested. Structures of newly synthesized compounds will be determined by spectroscopic methods, with special attention on 2D NMR techniques in structure elucidation. Synthesis of a number of new steroidal compounds is expected, where some of they would show significant antiproliferative activity. It is expected as well that novel synthesized bile acid derivatives would form micelles with high capacity for the inclusion of the guest molecules and with low hemolytic potential (low membranotoxicity). For those reasons they are expected to be potential biopharmaceutical agents.