ddt 10 Flashcards
( CHECK THE MECHANISM )
cholormethine becomes —- and the ring strain if this ion ring makes it —– and this is a —- reaction
- azidrine ion
- very reactive with a nuclephile
- SN2 reaction with nucleophile and elctrophile are in the same molecule
— is a cholomethine analogue the aromatic ring is — and it — the nculephilic strength of the nitrogen and makes it — reactive alkylating agent and — toxic
- cholorambucil
-electron withdrawing - decreases
- less reactive
- less and less side chain reactions
melphalan has an aromatic ring and is —- and mimics the —– and transported into the cells by —-
- less reactive alkylating agent
- amino acids phenalanine
- transport protein
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 —
- urethene
- electron withdrawing
- lowers
- estradiol
- hydrophobic
- cross the cell membrane
uricl mustard’s uricl ring is — which makes it — reactive and mimic a —- and concentrate in —-
- electron withdrawing
- less
- nucleic acid base
- fast growing cells
the effects of dna alkylation leads to —-
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
cyclophosphoamide is the —– and is —- pro drug and is — active
acrolein by product is associated with —-
- most commonly used alkylating anti cancer agent
- non-toxic
- orally
- toxicity
the prodrug nutosoureas decomposes in the body to from —
the alkylating agent causes — crosslinking between
alkylating agent
( CHECK STRUCTURE )
- inter strand between G-G or G-C
busulfan dna alkylating agent is a — compound used as — agent and causes —- by — reaction
( CJECK MEHCNAISM )
- synthetic
- anti cancer
- SN2
( guanine –> with -meSO3 which is a good leaving group and better than cl- )
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
- alkylating agent
the most common alkylating agent used for anti cancer
cyclophosphoamide
the most toxic anti cancer drug used in clinical use
mitomycin c
CC1065 is a — occurring agent and bind to —- of the dna and it alkylates —- and is — more active than cisplatin
- naturally
- minor groove of dna
- adenine
- 1000
—is 1000 more active than cisplatin
CC1065
— 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
tamoxifen
17B-estradiol ( so it needed to be blocked so cancer doesn’t occur )
— binds to oestrogen receptor binding site without fully activating the receptor and prevents — from binding
- tamoxifen
- 17Bestradiol
– is referred to as partial agonist
tamoxifen
5-flurouricl ( 5-FU) is an —- which are compounds that prevents the —-
- antimatbolites
- biosythesis of normal cells metabolites
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
-uracil
( basically uracil –> thymidine )
- fluorine
( basically 5flurouricle –> won’t lead to thymidine )
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
over expressed , antibiotic
— 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
monoclonal
these are useful for treatment of : breast cancer , colorectal and lymphoma
But the level of anti-cancer activity is usually — so they are often
used in —- with small molecule anticancer drugs.
low , combination
— is a humanised monoclonal antibody which targets HER-2 growth factor receptor which is over expressed on 25% of breast cancer
Herceptin
Herceptin is approved for treatment of HER-2 positive metastatic breast cancer with combination with the mitotic inhibitor —
pacilatixel
— is used for non-hodgkin lymphoma treatment
rituximab
—- chimeric monoclonal antibody against the protein CD20, which is primarily found on the surface of immune system B cells.
rituximab
rituximab destroys — and is used to treat diseases characterised by excessive number of them or dysfunctional such as lymphoma and leuckima
b - cells
are proteins created through the joining of two or more genes
that originally coded for separate proteins.
chimeric antibody
— is one of the more widely used combination chemotherapy regimes
R-CHOP
— is the first line of treatment for non-hodgkin lymphoma ( NHL)
R-CHOP
a course of R-CHOP involves — treatments separated by — with:
— monoclonal antibody
— guanine alkylating agent
— mitotic inhibitor
— dna intercalaror acting as topoisomerase II poison )
- rituximab
- cyclophosphamide
- vincristine
- doxorubicin
