OLIGONUCLEOTIDES WITH BORONATED PHOSPORUS BACKBONES

THE OBJECTIVE IS TO DEFINE NOVEL OLIGONUCLEOTIDES THAT HAVE PENDANT GROUPS CONTAINING BORON ATTACHED TO PHOSPHORUS IN THE PHOSPHODIESTER BACKBONE. SUCH BORONATED OLIGONUCLEOTIDES MAY FUNCTION AS DESIGNED RECOGNITION MOLECULES AND BIND TO SELECTED POLYNUCLEOTIDE SEQUENCES YET IMPART USEFUL CHARACTERISTICS. OF SPECIAL IMPORTANCE IS THEPOTENTIAL FOR THE BORONATED OLIGONUCLEOTIDES TO BE USED IN BORON NEUTRON CAPTURE THERAPY FOR THE TREATMENT OF CANCER. ADDITIONAL INNOVATIVE USAGE IS ANTICIPATED IN PREVENTING GENE EXPRESSION BY BLOCKING TRANSCRIPTION OR TRANSLATION OF MESSENGER RNA'S, PROVIDING A NEW WAY OF STUDYING GENE ACTION IN CELLS OF HIGHER ORGANISMS. BORONATED OLIGONUCLEOTIDES MAY BE DESIGNED TO BE MORE MEMBRANE SOLUBLETHAN NORMAL OLIGONUCLEOTIDES, THEREBY ENABLING THEM TO PASS THROUGH CELL MEMBRANES AND TO BE MORE STABLE IN CELLS. A RATIONALE FOR THE GENERAL SYNTHETIC APPROACH TO SUCH BORONATED OLIGONUCLEOTIDES IS PRESENTED, AS WELL AS PRELIMINARY EVIDENCE FOR THEIR EXISTENCE AND PLANS FOR A SYSTEMATIC EXPLORATION OF SUCH NOVEL COMPOUNDS. BORON DERIVATIVES OF NUCLEIC ACIDS MAY CONSTITUTE A NEW CLASS OF BIOLOGICAL MODIFIERS AND NEED TO BE TESTED AS VIRAL INHIBITORS, ANTINEOPLASTIC AGENTS, CELL-GROWTH INHIBITORS, AND EFFECTORS OF CELL DIFFERENTIATION.