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Pharmacology & Medical Chemistry II > Exam 3: Lecture 8, Medical Chemistry Cancer Drugs Part III > Flashcards

Exam 3: Lecture 8, Medical Chemistry Cancer Drugs Part III Flashcards

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1
Q

Purine Antimetabolites

A

analogs of purine guanine in which carbonyl group is replaced with thiocarbonyl group.

metabolized to deoxynucleoides by HPRTase

inhibit many enzymes involved in purine metabolism

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2
Q

Purine Antimetabolite uses

A

treatment of acute leukemias

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3
Q

Purine Toxicity

A

bone marrow suppression
nausea
vomiting

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4
Q

Enzymes Purine antimetabolites inhibit

A

Primary target: AMP and GMP biosynthesis

primary action is by inhibition of enzyme

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5
Q

important fact about Purine antimetabolites?

A

They are prodrugs

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6
Q

Sugar-modified pyrimidine analogs

A

Cytarabine

Gemicitabine

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7
Q

Cytarabine

A

Inhibits conversion of cytidylic acid to 2’deoxycytidylic acid

causes miscoding after being incorporated into DNA

rapidly deaminated in body into inactive uric derivative, can only be give continuous IV infusion

~3hr 1/2 life

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8
Q

Enzymes Cytarabine inhibits?

A

also inhibits both DNA and RNA polymerases and nucleotide reductase enzyme needed for DNA synthesis

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9
Q

Gemicitabine

A

excellent anti tumor activity in vivo against variety of murine solid tumors

must 1st be phosphorylated to active triphosphate analogue, incorporated into DNA and cause cell death

~19hr 1/2 life due to difluorination

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10
Q

What deactivates Gemicitabine?

A

deaminase

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11
Q

Antitumor Antibiotics

A

known for long time, rejected due to toxicity

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12
Q

Bleomycin isolated from….

A

Streptomyces verticillus

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13
Q

Key to Bleomycin anti tumor activity?

A

tendency to form metal chelates

in cells form chelate with iron Fe2+

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14
Q

Bleomycin MOA

A

Chelate affects redox potential such that bound oxygen is reduced, converting into reactive radical species, the Hydroxyl radical which then binds to DNA and degrades it

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15
Q

Anthracycline inhibit….

A

Topoisomerase II

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16
Q

Anthracyclines are effective against….

A

more types of cancer than any other class but can cause Cardiotoxicity

17
Q

Anthracycline MOA:

A

DNA intercalation followed by free radical damage to DNA,

Inhibitors top II -> form active Oxygen species -> DNA Damage

18
Q

Valrubicin is…

A

a semisynthetic analog of Doxorubicin and has been used to treat bladder cancer

19
Q

Antimitotic agents are….

A

molecules that target mitosis and inhibit cell division

20
Q

Well known antimitotic drugs are..

A

Taxanes and Vinca Alkaloids

Both effective but limited by development of drug resistance and significant neurotoxicity

21
Q

Vincristine and Vinblastine block mitosis by….

A

metaphase arrest by binding specifically with tubule and causing its depolymerization.

22
Q

Portions of Vinca Alkaloids that are essential for high affinity binding?

A

Vindeline

Catharamine

23
Q

Taxanes are…

A

very hard to synthesize because they have several chiral centers

produced semi synthetically

bind to B tubulin

24
Q

Taxol has how many chiral centers?

A

11

25
Q

What gives increased aqueous solubility for Docetaxel?

A

A Hydroxyl group

26
Q

Hydroxyurea info

A

LMW w/ good oral bioavailability

27
Q

Hydroxyurea MOA:

A

anticancer activity due to inhibition of ribonucleotide diphosphate reduction, leading to decreased levels of deoxyribonucleotides required for DNA synthesis

28
Q

What phase is Hydroxyurea specific for?

A

S Phase and causes arrest at the G1-S interface

29
Q

Antiestrogens nd Aromatase inhbitors

A

Tamoxifen

Anastrazole and Letrozole

30
Q

Tamoxifen is….

A

estrogen agonist/antagonist (Partial agonist) that is used in treatment fo estrogen dependent breast cancer

Metabolism produces active metabolite 4-hydroxytamoixifen

31
Q

Anastrazole and Letrozole are….

A

competitive inhibit of aromatase that selectively inhibit conversion of testosterone to estrogens in all tissues

32
Q

Which enzymes do Anastrazole and other triazoles inhibit?

A

Aromatase enzyme by binding of N-4 nitrogen of triazole ring with heme iron atom of CYP19 eynyze complex

33
Q

Anastrazole and Ketrozole are used for treatment of…

A

advanced breast cancer in postmenopausal woman w/ disease progression following tamoxifen therapy

Pharmacology & Medical Chemistry II (43 decks)

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