was used as an offensive weapon by the Germans during World War I, and the related nitrogen mustards investigations showed that the toxic gases had destroyed the blood’s white cells, which subsequently led to the discovery of drugs used in leukemia therapy.
Sulfur mustard gas
Anticancer drugs
6-Mercaptopurine
Paclitaxel(Taxol)
Cisplatin
first effective leukemia drug developed by George Hitchings and his technician, Gertrude Elion
6-Mercaptopurine
6-Mercaptopurine - first effective leukemia drug developed by George Hitchings and his technician, Gertrude Elion. By a process now termed
“rational drug design,”
Hitchings hypothesized that it might be possible to use antagonists to stop bacterial or tumor cell growth by interfering with (blank)in a similar way that sulfonamides blocked cell growth.
nucleic acid biosynthesis
“have only affinity for the receptors and no (zero) efficacy”. In other words, it will only inhibit the agonist to bind on the binding site by competitive antagonism
Antagonism
- gold standard against which new medicines are compared
Cisplatin
serves as a reference for the other anticancer agents.
Gold Standard
interferes with the growth of cancer cells by binding to DNA and interfering with the cells’ repair mechanism and eventually causes cell death. - It is used to treat many types of cancer, primarily testicular, ovarian, bladder, lung, and stomach cancers
Cisplatin
elucidated its structure
Alfred Werner
It was not until the early 1960s when a professor of biophysics and chemistry at Michigan State University, observed the compound’s effect in cell division, which prompted him to test cisplatin against tumors in mice
Barnett Rosenberg
The compound was found to be effective and entered clinical trials in 1971.
Barnett Rosenberg
Although cisplatin is still an effective drug, researchers have found second-generation compounds such as (blank) that have less toxicity and fewer side effects
carboplatin
in 1963, they discovered Paclitaxel (Taxol) at Research Triangle Park in North Carolina the structure of the compound was established in the year 1967
Monroe E. Wall and Masukh C. Wani
Taxol was isolated from extracts of the bark of the
Pacific yew tree
n the year 1967 Taxol was isolated from extracts of the bark of the Pacific yew tree (scientific name: Taxus brevifolia). The extract showed potent
anticancer activity
Working at Albert Einstein College of Medicine in New York studied the mechanism of how Taxol can kill the cancer cells.
➢ Susan Horwitz