G08: Sciences - Synthetic Materials: Medication

Over twenty-one million chemical compounds were known as of 2003. Most have been synthesized by chemists; only a small fraction of these are compounds isolated from natural sources. The final proof of a naturally occurring compound's structure is established by synthesizing the compound from simpler molecules by means of identifiable and reproducible reactions.

When Arthur S. Barclay stuffed a bag with 15 lb of twigs, needles, and bark from Pacific yew trees in a forest near Mount St. Helens some 43 years ago, he couldn't have known that history was about to be made.

Monroe Wall, Mansukh Wani and colleagues at the Natural Products Laboratory of the Research Triangle Institute discovered and elucidated the structure Taxol® and camptothecin, two life-saving compounds for the treatment of cancer. These natural products kill cancer cells via unique mechanisms of action and in ways scientists had not previously imagined.

Paclitaxel, the most well-known natural-source cancer drug in the United States, is derived from the bark of the Pacific yew tree (Taxus brevifolia) and is used in the treatment of breast, lung, and ovarian cancer, as well as Kaposi's sarcoma.

National Cancer Institute (NCI)-funded researchers unlocked the Pacific yew tree’s potential to treat cancer and developed the lifesaving compound paclitaxel (Taxol).
Taxol, an antimitotic agent used to treat cancer, blocks cancer cell growth by stopping cell division, resulting in cell death.
An NCI-funded clinical trial found that 30 percent of patients with advanced ovarian cancer responded positively to Taxol treatment.

Research by German scientists to discover a substitute for quinine led to the synthesis in 1934 of Resochin (chloroquine) and Sontochin (3-methyl-chloroquine). These compounds belonged to a new class of antimalarials, the four-amino quinolines. The German research went no further and the formula for Resochin was passed to a US sister company.

Aspirin has had a long history as a pain reliever. But only in the 1970s did scientists begin to uncover its chemical secrets.

And the daddy of all semi-synthetic drugs is aspirin. Back in the 18th century, an Oxfordshire clergyman named Edward Stone pioneered the use of willow bark in treating fevers; the bark contained a molecule called salicin, which in the body is transformed into the active compound, salicylic acid.

The German chemist Felix Hoffmann famously synthesized two drugs: aspirin, one of the most widely beneficial drugs ever, and heroin, one of the most harmful of illegal substances. These two drugs represent the efforts of late-19th-century chemists to create new substances that could be used as medicines, not just to isolate active ingredients from natural products or to imitate them.

In 1935, in Minshall Laboratory, DePauw alumnus Percy L. Julian (1899-1975) first synthesized the drug physostigmine, previously only available from its natural source, the Calabar bean. His pioneering research led to the process that made physostigmine readily available for the treatment of glaucoma. It was the first of Julian’s lifetime of achievements in the chemical synthesis of commercially important natural products.

A steroid chemist and an entrepreneur, Percy Julian ingeniously figured out how to synthesize important medicinal compounds from abundant plant sources, making them more affordable to mass-produce.

Learn about chemist Percy Julian's work to synthesize cortisone. Julian's work made cortisone—a steroid used to treat rheumatoid arthritis—more easily accessible to millions of patients. Julian knew from earlier studies that plants and animals produced steroids with the same carbon-ring structure, so he isolated large quantities of molecules that closely resembled human cortisone from a cheap and abundant plant source—soybeans.