Anti-Cancer

Intercalating agent

dialkylating agent nitrogen mustard structure

dialkylating agent platin structure

purines - guanidine and adenosine

pyridines - thymine and cytosine

Folic acid analogue - inhibit DHFR

HORMONAL

anti-metabolites - vinca

Anti-metabolite - paclitaxel taxane based

kinase inhibitor

intercalating agent MOA

MOA: Planar aromatic rings that SLIDE between DNA base pairs, distorting the DNA helix and inhibiting replication/transcription

alkylating agent MOA

MoA: Covalently bind to nucleophilic DNA sites, causing mispairing or cross-linking (e.g. guanine to cytosine usually, now to thymine)→ inhibition of replication. Add an alkyl to DNA

anti-metabolites MOA

MoA: Mimic natural nucleotides, disrupting nucleotide biosynthesis or incorporation - disrupt mitosis

what does folic acid analogues inhibit?

DHFR

hormone analogues

MOA: administering opposing gender’s hormones

Drugs acting on structural proteins MOA

MOA: Disrupt cell mitosis by Ix with tubulin - (structural protein and building block for microtubules which are polymerised and depolymerised during cell division) - ANTIMITOTIC AGENT

Paclitaxel (taxane based) MOA

MoA: Promotes tubulin polymerisation → prevents depolymerisation (stimulate formation of spindle and prevent disassembling - as need to form and dissemble)

Vinca alkaloids MOA

• MoA: Bind tubulin and induces depolymerisation → prevent polymerisation → spindle collapse

kinase inhibitors moa

MOa: Inhibit ATP-binding site of overactive protein kinases involved in cancer cell signalling.

types of kinase inhibitors

• Type I: Active conformation –  bind to ATP binding site and block access to ATP - Gefitinib, Erlotinib

• Type II: Inactive conformation – bind to enzyme and stabilise inactive conformation -  Imatinib, Nilotinib - more selective but random mutation risk

• Allosteric/Irreversible: Trametinib, Afatinib, Ibrutinib - contain NCOC=C (amide to alkyne)

What drugs are the only ones with halogens

kinase inhibitors and alkylating agents

what drugs undergo bioactivation

pro-drugs - anti-metabolites usually, alkylating agents

What drugs are enzyme inhibitors

antimetabolites and kinase inhibitors