Medicinal Chemistry

carcinogenic (cancer-causing) substances through precisely the same mechanism. There is a fine line between anticancer compounds ...

synthesized by treating p-aminophenyl butyric acid with ethylene oxide, followed by thionyl chloride. Although the nitrogen must ...

A nitrogen mustard prodrug, cyclophosphamide (7.65), was synthesized in the hope of exploiting the high level of phosphoramidase ...

ion in an excellent leaving group. Busulfan is synthesized by treating 1,4-butanediol with methanesulfonyl chloride in the prese ...

7.8.1.3 Antimetabolites Antimetabolite inhibitors of DNA synthesis act by the competitive or allosteric inhibition of a number o ...

acid to AMP and GMP are also inhibited. Both 6-mercaptopurine and 6-thioguanine have been used in the treatment of acute leukemi ...

7.8.1.4 DNA Topoisomerase Inhibitors DNA is a topologically constrained molecule because the ends of the circular double helix a ...

They cause substantial DNA damage in tumor cells, preventing tumor growth. Topotecan has been evaluated in metastatic ovarian ca ...

7.8.2.2 Synthetic Anti-Transcription Agents Another group of agents that interfere with DNA transcription are the platinum compl ...

are assembled at one of their ends and disassembled at the other. The microtubules are hollow tubes built from 13 dimers of two ...

7.8.4 Targeting Nucleic Acids: Drug Design Approaches 7.8.4.1 Designing Cell-Cycle-Specific Agents In designing drugs to target ...

cancer chemotherapy drug design are exploiting non-nucleic acid strategies. These new directions include: Angiogenesis inhibito ...

Ras protein, for example, is central amongst the many oncogene(“cancer-producing gene”) encoded proteins that relay signals from ...

conversion of the drug from a nontoxic form to a tumor-killing form. This conversion is achieved uniquely within the tumor cells ...

of malignancy in a neoplasm. Likewise, metastasis also unequivocally marks a tumor as malignant, since benign neoplasms cannot m ...

area (e.g., tongue, skin of face), then the tumor will be detected early. If the site of origin is in a hidden area (e.g., ovari ...

blocks as the host that it is destroying. Therefore, a tumor is “self acting as nonself.” Drugs engineered to attack tumor nucle ...

This observation opens a window of opportunity, enabling a partially selective targeting of tumor cells in preference to host ce ...

H. Meyer (1983). Structure–activity relationships in calcium antagonists. In: L. R. Opie (Ed.). Calcium Antagonists and Cardiova ...

8 Nonmessenger Targets for Drug Action II Endogenous macromolecules 465 8.1 Endogenous Macromolecules: Relevant Biochemistry If ...