Problem 4 Duocarmycin B1 and Duocarmycin B2 are both minor groove alkylating age

Question

Problem 4

Duocarmycin B1 and Duocarmycin B2 are both minor groove alkylating agents. However, like most

alkylating agents these drugs do not undergo simple one-step SN2 substitution as part of the reaction

pathway. Propose a mechanism that explains how these drugs bind to DNA.

Problem 5

Cytarabine is a chemotherapy agent used mainly in the treatment of

cancers of white blood cells such as acute myeloid leukemia (AML) and

non-Hodgkin lymphoma.

What class of drugs would Cytarabine belong to and describe the

mechanism of action of this drug.

BCX4430 is active against the Ebola virus. What class of drugs would BCX4430 belong to and

suggest a mechanism of action of this drug.

Explanation / Answer

4.

Duocarmycin B1 and Duocarmycin B2 are both minor groove alkylating agents. However, like most alkylating agents these drugs do not undergo simple one-step SN2 substitution as part of the reaction. These alkylating agents bind to minor groove and bind at N3 position of adenine and alter its structure. They also bind to minor groove by noncovalent binding.

5.

Cytarabine is a chemotherapy agent used mainly in the treatment of cancers of white blood cells such as acute myeloid leukemia (AML) and non-Hodgkin lymphoma. Cytarabine is a class of chemotherapeutic drugs called antimetabolites. Antimetabolites are drugs that very similar to normal substances within the cell. When the drug incorporated into cells or into the cellular metabolism, the cells are unable to divide. Antimetabolites are cell-cycle specific. They attack cells at very specific phases in the cycle. Antimetabolites are classified according to the substances with which they interfere.

BCX4430 is active against the Ebola virus. BCX4430 is a novel synthetic adenosine analogue that inhibits infection of distinct filoviruses in human cells. Biochemical, reporter-based and primer-extension assays indicate that BCX4430 inhibits viral RNA polymerase function, acting as a non-obligate RNA chain terminator. Post-exposure intramuscular administration of BCX4430 protects against Ebola virus and Marburg virus disease in rodent models. In addition, BCX4430 exhibits broad-spectrum antiviral activity against various viruses, including bunyaviruses, arenaviruses, paramyxoviruses, coronaviruses and flaviviruses.

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