In this volume, internationally renowned chemists recount their roles in the progress of chemistry research toward elucidation of biological processes. Beginning with a historical perspective on the development of X-ray crystallography, the reader is regaled with first-hand accounts of research milestones. Included are descriptions of the cutting-edge nuclear-magnetic-resonance and electron-paramagnetic-resonance spectroscopic techniques, the dynamics of ultra-fast reactions, and the central problem of molecular oxygen activation in biological processes. The roles of chiral auxiliaries in organic synthesis and of photochemistry in natural product synthesis are told, and innovations in combinatorial synthesis approaches are described. Contemporary issues in molecular recognition and modulation of molecular function are addressed, concluding with a missive regarding how the frontiers of medical ethics may be breached by molecular manipulations. The contributors, who number among the finest scientists in the world, including two Nobel Prize winners, are Peter B. Dervan, Jack D. Dunitz, Christian Griesinger, Jean-Marie Lehn, Thomas F. Prisner, Gerhard Quinkert, Peter G. Schultz, Helmut Schwarz, Dieter Seebach, and Ahmed Zewail. Additionally, there is a prologue by Albert Eschenmoser, for whom this collection was conceived, and an epilogue that contains facsimiles of notes from his landmark lecture 'Synthesis of Co-Enzyme B12: A Vehicle for Teaching Organic Synthesis'. This book is definitely a must for all who want to read, or to read again, where we stand in our chemical comprehension of the fascinating relationship between chemical structure and biological processes, how we got here, and what the future might hold.