28 Questions
What is the main focus of the lecture on Cancer Chemotherapeutic Agents?
Discussing the therapeutic properties of reductively activated anticancer agents
Why do areas of hypoxia and necrosis often develop in tumor tissue?
Tumor cells are chaotic and have sluggish blood flow
Which characteristic distinguishes normal vasculature from tumor vasculature?
Dilated and tortuous vessels
What is the significance of DNA intercalating agents in cancer treatment?
They disrupt DNA structure in tumor cells
Which type of anticancer agents are reductively activated, such as mitomycin C?
DNA intercalating agents
What structural units are present in Mytomycin C?
Quinone and aziridine
Which type of cancer is porfiromycin in phase III trials for according to the text?
Head and neck cancer
What is the main limitation mentioned in the text regarding the effectiveness of Mitomycin C and similar compounds?
They require bioreductive activation
What is the active species formed after the reduction of Mitomycin C?
Hydroquinone
How does Mitomycin C react with DNA according to the text?
Forms bridges between two complementary DNA strands
What is the mechanism of action of Mytomycin C's indole derivative?
Creates electrophilic iminium species
Which structural feature is most common in compounds like Mitomycin C?
'Quinone unit'
Which type of bonding is primarily responsible for the stabilization of the intercalated complex of doxorubicin with DNA?
Electrostatic interactions
Which of the following processes does doxorubicin NOT participate in to cause DNA damage?
Causing the formation of hydrogen peroxide (H2O2)
Which of the following factors contributes to doxorubicin-induced cardiotoxicity?
The presence of Fe2+, which converts H2O2 to the highly toxic .OH radical through the Fenton reaction
Which of the following statements best describes dexrazoxane in relation to doxorubicin-induced cardiotoxicity?
Dexrazoxane is an antioxidant and iron chelator that minimises cardiac toxicity caused by doxorubicin
Which enzyme is involved in the conversion of H2O2 to water and oxygen in the presence of dexrazoxane?
Catalase
Which of the following does NOT contribute to the mechanism of action of doxorubicin in treating cancer?
Direct binding to and inhibition of cell membrane proteins, leading to cell death
What is a common structural feature of mitomycin analogs designed for activity in nonhypoxic cells?
Aminoethylene disulfide side chain
Which compound is exemplified by KW-2149, known to cause interstrand DNA cross-links and DNA–protein cross-links?
KW-2149
What is the process through which DNA intercalating agents interact with DNA?
Intercalation
What is the term used to describe the perpendicular insertion of aromatic ring systems between DNA base pairs?
Intercalation
Mitoxantrone is more efficient as a DNA intercalator due to its interaction with which part of the DNA?
Sugar phosphate backbone
Which type of interactions stabilize the complex formed between a DNA intercalating drug and DNA?
Van der Waals, π- π stacking interactions, ionic interactions, hydrogen bonding
What structural characteristic makes cationic species more efficient DNA intercalators?
+vely charged groups that interact with DNA sugar phosphate backbone
Which molecules are typically distorted by the insertion of DNA intercalators between base pairs?
-vely charged sugar phosphate backbone
What specific structural changes induced by DNA intercalation interfere with the function of DNA-associated proteins?
Unwinding of the double helix
What term best describes the process where DNA undergoes a conformational change involving an increase in vertical separation between base pairs upon intercalation?
Unwinding
Test your knowledge on reductively activated anticancer agents like mitomycin C, DNA intercalating agents, and tumor hypoxia. Explore the therapeutic properties, cytotoxicity mechanism, and rational for use of these agents in cancer treatment.
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