Alkylating agents

Question 1

One of the simplest nitrogen mustards used for testis cancer.

Answer 1

Mechlorethamine

Question 2

At which position does reactive metabolite alkaylates DNA

Answer 2

N-7 position of guanine covalently and donate electrons.

Question 3

Bifunctinal alkylating agents

Answer 3

Cause DNA crosslinks which leads to miscoding, depurination(removal of guanine), stand break, or cross links. Those are very difficult to fix.

Question 4

Alkylating agents

Answer 4

Proliferation-dependent, cell cycle phase non-specific anticancer drugs whose functin depends on how many leaving group; thus, how many bonds, it has.

Question 5

Phosphoramide mustard

Answer 5

Metabolized Cyclophosphamide and acrolein(from cegarette) by P450. cross-link with DAN and, usually, used with other drugs.

Question 6

Cisplatin

Answer 6

Form covalent bonds with guanine and form interstrand cross-link. it can also binds with gluathione which can inactivate alkylating agents.

Question 7

Resistance and Toxicity of alkylating agents

Answer 7

Increased inactivation and DNA repair, and decrease in activation of drugs / Affects Hematopoietic system, GI tract, Gonads, and may leads to secondary malignancies.