Designing Anti-Tumor Drugs Using Natural and Synthetic Agents

Designing Anti-Tumor Drugs Using Natural and Synthetic Agents
By:Herman L. Holt, Jr.
University of North Carolina, Asheville

Medicinal Chemistry Folklore
Famous for Synthesis and Discovery of the Mechanism of Action of:
Indomethacin
Sulindac
Diflunisal
Other anti-inflammatory-analgesic (NSAIDS) and immunoregulators
More than 210 U.S. Patents and scientific publications


* Medicinal Chemistry is defined as an interdisciplinary science situated at the interface of organic chemistry and life sciences (such as biochemistry, pharmacology, molecular biology, immunology, pharmacokinetics and toxicology) on one side and chemistry-based disciplines (such as physical chemistry, crystallography, spectroscopy and computer-based information technologies) on the other.

Chemistry based disciplines
Organic Chemistry
Life Sciences
Medicinal Chemistry
Definition and Objectives
Challenges for Medicinal Chemistry
TUBULIN
* Globular Protein
* Taxoid Site
* Vanca Alkaloid
Domain
* Colchicine Site
MICROTUBULES
* Tubulin Polymers
MITOTIC SPINDLE
* Composed of Microtubules and associated proteins
* Needed for cellular division
* Tubulin Polymers

What is the MTT assay?
CISPLATIN
* Anti-cancer agent
* Ovarian
* Testicular
* Lung
* Breast
* Cleaves DNA

TAXOL
* Anti-cancer agent
* Pacific Yew Tree
* Ovarian
* Testicular
* Lung
* Breast

VANCOMYCIN
COLCHICINE
COMBRETASTATIN
HETEROCYCLE ANALOGS OF COMBRETASTATIN
COMBRETASTATIN AND TRIAZOLE SYNTHESIS
AZIRIDINE ANALOGS OF COMBRETASTATINS
AZIRIDINE TYPE ANALOGS OF COMBRETASTATINS
MITOMYCINS
REFERENCES

Designing Anti-Tumor Drugs Using Natural and Synthetic Agents.ppt