COURSE OBJECTIVE
To acquaint students with the basic principles of action of antitumor drugs that contain heterocyclic nuclei in their structure. Division of antitumor drugs according to the manner and mechanisms of their biological action. Special emphasis on drugs whose mechanism of biological action is based on the interaction with DNA and RNA biomolecules.
COURSE IMPLEMENTATION PROGRAM
WEEK 1
Introduction and basic principles of chemotherapy. The role of chemistry in chemotherapy. Basic division of antitumor drugs according to the mode of their biological action. Antimetabolites.
WEEK 2
Antitumor drugs that inhibit the action of hormones. Antiandrogens. Estrogen inhibitors.
WEEK 3
Antitumor drugs whose action is based on radical mechanisms. Anthracyclines and their analogues. Actinomycin D. Photodynamic antitumor therapy.
WEEK 4
DNA alkylating and non-alkylating antitumor drugs. Nitrogen mustard derivatives. Aziridines. Epoxies. Nitrozouree. Triazene. Methylhydrazines. 1,3,5-triazines. Complexes of organic molecules with platinum.
WEEK 5
Alkylating and non-alkylating DNA groove binders. Netropsin and distamycin. Hoechst 33258. Mitomycin. Pyrrolo (1,2-a) benzodiazepines.
WEEK 6
DNA intercalators. Basic principles of intercalation in DNA and RNA. Elliptin and analogues. Actinomycins. Quinoline derivatives. Intercalators with indole and naphthalimide nuclei. Acridini.
WEEK 7
1. Written partial test.
WEEK 8
Antitumor drugs as topoisomerase I and II inhibitors. Drugs that act as toxins on topoisomerases. Catalytic topoisomerase inhibitors.
WEEK 9
Tubulin and microtubule inhibitors.
WEEK 10
The role of protein kinases in chemotherapy. Tyrosine kinase inhibitors.
WEEK 11
Other principles of targeted chemotherapy.
WEEK 12
Antitumor drugs isolated from natural products.
WEEK 13
An overview of the most significant commercial antitumor drugs used in chemotherapy today. Glivec. Taxol.
WEEK 14
2. Written partial test.
DEVELOPMENT OF GENERAL AND SPECIFIC COMPETENCIES OF STUDENTS:
Groups of antitumor drugs with respect to the mechanism of their biological action in chemotherapy. Knowledge of specific structural characteristics of individual groups of heterocyclic antitumor drugs. Newer methods used in chemotherapy (inhibitors of specific enzymes).
STUDENTS 'TEACHING OBLIGATIONS AND THEIR PERFORMANCE:
Students are required to attend lectures.
Students are required to do all the lab exercises.
Students are required to access knowledge tests and partial test (related to laboratory exercises).
CONDITIONS FOR OBTAINING A SIGNATURE:
80% attendance at lectures.
Completed laboratory exercises, prepared and submitted papers, passed the final colloquium in laboratory exercises.
TEACHING METHODS:
Lectures (ex cathedra).
Lecture through e-learning.
Laboratory exercises (practical work in groups under the supervision of an assistant).
Consultations by arrangement with students.
METHOD OF EXAMINATION OF KNOWLEDGE AND EXAMINATION:
Partial test from laboratory exercises.
2 mandatory written partial tests during the semester (60% of points on each of the tests brings exemption from the oral exam).
Written exam (requires 55% points to pass).
Oral exam.
METHOD OF MONITORING THE QUALITY AND PERFORMANCE OF COURSES:
Student survey.
METHODOLOGICAL PREREQUISITES:
Passed the exam in Organic Chemistry in Drug Development (if the student enrolled in that course).
COURSE LEARNING OUTCOMES:
1. To identify and distinguish groups of heterocyclic antitumor drugs according to the mechanism of their biological action.
2. To review critically and interpret some of the important biological processes in the body associated with the formation of tumor cells.
3. To recognize the function of certain highly selective enzymes whose action is associated with the formation of tumor cells.
4. Get acquainted with the latest principles of antitumor chemotherapy.
5. To apply the acquired knowledge and show the ability in the synthesis of potential antitumor drugs.
LEARNING OUTCOMES AT PROGRAM LEVEL:
1. To connect basic facts, concepts, chemical principles and theories related to advanced areas of chemistry and chemical technologies
2. To apply more complex chemical principles that continue the basic knowledge of chemistry acquired in undergraduate study
3. To demonstrate the ability to work independently with minimal mentoring
4. To use advanced laboratory procedures and instrumentation within chemical synthesis and analysis
5. To plan independently experiments with self-criticism in the evaluation of experimental procedures and results
TEACHING UNITS WITH ASSOCIATED LEARNING OUTCOMES AND EVALUATION CRITERIA
Teaching unit
1. Antitumor drugs whose biological action is associated with metabolic processes, hormones and radical mechanisms in the human body.
Learning outcomes:
- to define groups of heterocyclic antitumor drugs according to the specified teaching unit
- to identify characteristic drugs from each of these groups
- to identify and analyze the mechanisms of action of these groups of antitumor drugs
Evaluation criteria:
- to know the group of antitumor drug according to the given structure of the drug
- to determine the structural characteristics of a particular group of antitumor drugs
- to understand the differences in the mechanisms of action between individual groups of drugs
2. Antitumor drugs whose biological action is associated with DNA / RNA biomacromolecules.
Learning outcomes:
- to define and list groups of antitumor drugs with regard to the way of interaction with biomacromolecules DNA / RNA
- to know the mechanism of biological action of intercalators, groove binders and alkylating agents
- to identify the most well-known drugs from the above groups of antitumor drugs
Evaluation criteria:
- to know the group of antitumor drug according to the given structure of the drug
- to interpret the structural characteristics of intercalators, groove binders and alkylating agents
- to understand the difference between the mechanisms of action of groove binders, intercalators and alkylating agents
3. Antitumor drugs whose biological action is associated with the inhibition of highly selective enzymes.
Learning outcomes:
- to get acquainted with the function of certain enzymes whose action is associated with the formation of tumor cells
- to define groups of antitumor drugs with regard to the inhibition of certain highly selective enzymes
- to identify and analyze the mechanism of action of a particular group of drugs from this group
Evaluation criteria:
- to know all highly selective enzymes whose action is associated with the formation of tumor cells
- to know the group of antitumor drug according to the given characteristic structure
- to understand the main differences between the modes of biological action of individual groups from this group of antitumor drugs
4. The latest principles of antitumor chemotherapy.
Learning outcomes:
- to get acquainted with the basics of the latest principles of antitumor chemotherapy
- to identify and analyze groups of antitumor drugs from this group
- to get acquainted with the differences of modern principles of antitumor chemotherapy in relation to the previously mentioned mechanisms of action of heterocyclic antitumor drugs
Evaluation criteria:
- to know the groups of drugs whose mechanism is based on the latest principles of antitumor chemotherapy
- to understand the differences between the latest principles of antitumor chemotherapy
- to define the structural characteristics of individual groups from this group of antitumor drugs
- to know the importance and differences of modern principles of antitumor chemotherapy in relation to the previously mentioned group of heterocyclic antitumor drugs
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C. Avendano, J. C. Menéndez, MEDICINAL CHEMISTRY OF ANTICANCER DRUGS, Elsevier B.V., 2008.
D. E. Thurston, CHEMISTRY AND PHARMACOLOGY OF ANTICANCER DRUGS, CRS Press, 2007.
M. Mintas, S. Raić-Malić, MEDICINSKA KEMIJA, Medicinska naklada, Zagreb 2009.,
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J. R. Hanson, CHEMISTRY AND MEDICINES, RSC Publishing, Cambridge, 2006.
R. R. Nadendla, PRINCIPLES OF ORGANIC MEDICINAL CHEMISTRY, New Age International, New Delhi, 2005.,
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