ddt 10

Question 1

( CHECK THE MECHANISM )
cholormethine becomes —- and the ring strain if this ion ring makes it —– and this is a —- reaction

Answer 1

• azidrine ion
• very reactive with a nuclephile
• SN2 reaction with nucleophile and elctrophile are in the same molecule

Question 2

— is a cholomethine analogue the aromatic ring is — and it — the nculephilic strength of the nitrogen and makes it — reactive alkylating agent and — toxic

Answer 2

• cholorambucil
  -electron withdrawing
• decreases
• less reactive
• less and less side chain reactions

Question 3

melphalan has an aromatic ring and is —- and mimics the —– and transported into the cells by —-

Answer 3

• less reactive alkylating agent
• amino acids phenalanine
• transport protein

Question 4

estramustine has a —- group which is electron — which mean it — the nucleophilic strength of the nitrogen. the alkylating group is attached to — and steroid is —- which makes it able to —

Answer 4

• urethene
• electron withdrawing
• lowers
• estradiol
• hydrophobic
• cross the cell membrane

Question 5

uricl mustard’s uricl ring is — which makes it — reactive and mimic a —- and concentrate in —-

Answer 5

• electron withdrawing
• less
• nucleic acid base
• fast growing cells

Question 6

the effects of dna alkylation leads to —-

Answer 6

miscoding
example:
normal base pairing as c - g
guanine prefers the veto tautomer and guanine is hydrogen bond acceptor/donor/donor
but in abnormal base pairing , the alkylated guanine prefers enol tautomer and the alkylated guanine is hydrogen bond donor/acceptor/ donor

Question 7

cyclophosphoamide is the —– and is —- pro drug and is — active
acrolein by product is associated with —-

Answer 7

• most commonly used alkylating anti cancer agent
• non-toxic
• orally
• toxicity

Question 8

the prodrug nutosoureas decomposes in the body to from —
the alkylating agent causes — crosslinking between

Answer 8

alkylating agent
( CHECK STRUCTURE )
- inter strand between G-G or G-C

Question 9

busulfan dna alkylating agent is a — compound used as — agent and causes —- by — reaction
( CJECK MEHCNAISM )

Answer 9

• synthetic
• anti cancer
• SN2
  ( guanine –> with -meSO3 which is a good leaving group and better than cl- )

Question 10

mitomycin is a prodrug activated in the body to from —- and is the most toxic anticancer drugs in the clinical use and the mode of action is dna alkylation

Answer 10

• alkylating agent

Question 11

the most common alkylating agent used for anti cancer

Answer 11

cyclophosphoamide

Question 12

the most toxic anti cancer drug used in clinical use

Answer 12

mitomycin c

Question 13

CC1065 is a — occurring agent and bind to —- of the dna and it alkylates —- and is — more active than cisplatin

Answer 13

• naturally
• minor groove of dna
• adenine
• 1000

Question 14

—is 1000 more active than cisplatin

Answer 14

CC1065

Question 15

— is an angent that antagonise the action of oestrogens and are interest for treatment of oestrogen dependent breast cancer .
— is a steroid hormone that promotes the growth of certain tissues

Answer 15

tamoxifen
17B-estradiol ( so it needed to be blocked so cancer doesn’t occur )

Question 16

— binds to oestrogen receptor binding site without fully activating the receptor and prevents — from binding

Answer 16

• tamoxifen
• 17Bestradiol

Question 17

– is referred to as partial agonist

Answer 17

tamoxifen

Question 18

5-flurouricl ( 5-FU) is an —- which are compounds that prevents the —-

Answer 18

• antimatbolites
• biosythesis of normal cells metabolites

Question 19

structurally designed compounds based on the experimental observations that tumor cells prefer use — for sytheis of the dna base thymidine using the biosynthetic pathway not used by normal cells.
So the presence of — at key position prevents the thymidine biosynthesis

Answer 19

-uracil
( basically uracil –> thymidine )
- fluorine
( basically 5flurouricle –> won’t lead to thymidine )

Question 20

Cancer cells have altered plasma membranes that contain
distinctive antigens which are —-
when compared to normal cells.
this allows the possible use of — against diseases

Answer 20

over expressed , antibiotic

Question 21

— antibodies have been produced for several tumour
associated antigens and can act to activate the body’s immune
response to direct killer cells against the tumour

Answer 21

monoclonal
these are useful for treatment of : breast cancer , colorectal and lymphoma

Question 22

But the level of anti-cancer activity is usually — so they are often
used in —- with small molecule anticancer drugs.

Answer 22

low , combination

Question 23

— is a humanised monoclonal antibody which targets HER-2 growth factor receptor which is over expressed on 25% of breast cancer

Answer 23

Herceptin

Question 24

Herceptin is approved for treatment of HER-2 positive metastatic breast cancer with combination with the mitotic inhibitor —

Answer 24

pacilatixel

Question 25

— is used for non-hodgkin lymphoma treatment

Answer 25

rituximab

Question 26

—- chimeric monoclonal antibody against the protein CD20, which is primarily found on the surface of immune system B cells.

Answer 26

rituximab

Question 27

rituximab destroys — and is used to treat diseases characterised by excessive number of them or dysfunctional such as lymphoma and leuckima

Answer 27

b - cells

Question 28

are proteins created through the joining of two or more genes
that originally coded for separate proteins.

Answer 28

chimeric antibody

Question 29

— is one of the more widely used combination chemotherapy regimes

Answer 29

R-CHOP

Question 30

— is the first line of treatment for non-hodgkin lymphoma ( NHL)

Answer 30

R-CHOP

Question 31

a course of R-CHOP involves — treatments separated by — with:
— monoclonal antibody
— guanine alkylating agent
— mitotic inhibitor
— dna intercalaror acting as topoisomerase II poison )

Answer 31

• rituximab
• cyclophosphamide
• vincristine
• doxorubicin