Single-Course English 5 ECTS

Advanced Medicinal Chemistry

Overall Course Objectives

To expand students’ understanding of central topics and challenges in medicinal chemistry. To understand and apply concepts from modern medicinal chemistry and chemical biology.

Learning Objectives

  • Demonstrate familiarity with methods for analyzing metabolites and modulating oxidative metabolism; as well as recognize and predict reactive metabolites.
  • Suggest relevant use of stable and radioactive isotopes in drug development and diagnostics
  • Explain limitations and possibilities for radioactive labeling of molecules in drug discovery, diagnostics and treatment
  • Describe modern principles of prodrug design and apply them to suggest more selective strategies for treating different diseases
  • Apply knowledge of target classes to design a screening campaign, including assays and required techniques
  • Explain the principles behind the design of larger collections of compounds and hits and assess their quality in different stages of a drug discovery pipeline
  • Describe and apply state-of-the-art and emerging strategies for drug design and development
  • Explain the importance of target identification and validation in a drug discovery pipeline
  • Describe and apply state-of-the-art and emerging strategies for immuno-oncology

Course Content

Lectures and discussions about topics within modern medicinal chemistry, including:

Metabolic reactions, hotspots and use of isotopic labeling to study metabolites.

Principles of radiochemistry and how radioactive isotopes can be used in medicinal chemistry, including drug development and for diagnostic imaging (PET, SPECT).

Modern concepts for the design and synthesis of prodrugs will be discussed, including tissue-selective activation mechanisms (redox, light, enzymatic, acidic).

Different strategies typically employed to design a successful assay will be outlined, and students will be able to suggest suitable screens for diverse target types (e.g. enzyme active site, protein-protein interaction) and target location (cytosolic or membrane-bound).

The properties that make a molecule a good hit, lead, tool and candidate will be discussed, with an emphasis on the fact that the quality of compounds in a screening library has a profound impact on the hits that can be identified and progressed through the drug discovery process.

Strategies to identify and validate targets will be outlined. The importance of this crucial step in the drug discovery process will be discussed with recent examples from the literature.

A series of next-generation therapeutics will be presented, including strategies for targeted protein degradation, photoactivatable drugs, carbohydrate-based therapeutics, and stapled peptides.

Current methods and trends in immuno-oncology will be discussed.

Recommended prerequisites

26426, Introduction to Medicinal Chemistry

Teaching Method

Lectures, group discussions and problem solving

Limited number of seats

Minimum: 10.

Please be aware that this course will only be held if the required minimum number of participants is met. You will be informed 8 days before the start of the course, whether the course will be held.

See course in the course database.





13 weeks




DTU Lyngby Campus

Course code 26446
Course type Candidate
Semester start Week 5
Semester end Week 19
Days Mon 13-17

7.500,00 DKK

Please note that this course has participants limitation. Read more