Med Chem, Natural Products

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natural prouducts:

herbal remedies::

-- of compound from plants, herbs, veggies

content of -- compoundn may ----

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mixture

active

vary

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drugs are --- agents

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single

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drugs are defined ----- entities

has --- molecules

isolated form --- -----

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defined

small

biological source

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methods of learning active compound

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pc pes

icp-ms

taxonomic id

mycotoxins: carcinogenic, tetrogenic, neurotoxin

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what's not safe for pregnancy

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volatile oils

herbal teas: caffeine

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use of gingko

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senile dementia

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avoid what part of of ginkgo

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avoid fruit pulp and seeds

ginkgotoxic

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gingseng use:

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stress and fatigue

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prob w/ gingseng

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differnt types, so possible diffenent metabolites

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active part of ginkgo

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ginkolides a-c

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diet supplements are exempt from regulation as drugs provided they are not marketed for the

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dx

tx

cure

prevention

of disease

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botancical dietary supplements are exempt from --- ---- ---

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good manufacturing proceees

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diet supplements doen require proof of ---

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efficacy

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how is safety determined of diet supplements

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thy self-regulation by manufacturer

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name some concerns form diet supplements

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contamination w/ pesticides, herbicides, heavy metal

use of incorrect parts of the plant

misid of plant species

inter-intra-species variation

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use of echinacea

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antiseptic activity

antiviral activity

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activity of echinacea due ot

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carbohydrates

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st john's wort use dfor

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anxiety

depression

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active part of st john's

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hyperricin

hyperforin

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kava used for

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muscle relant

anticonvulsant

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active part of kava

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a-quinone

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pennyroyal oil used for

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abortifacient

alleviates menstrual symptoms

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active part of pennyroyal oil:

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epoxide

has known toxicities

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sassfras oil used for

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diuretic

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active part of sassafras oil

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carbocation

known toxicities

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aristolochia fangchi used for

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weight loss remedies

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active part of aristolochia-fangchi

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nitrenium ion

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antioxidant used for

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increase antioxidative and carcinogen-detoxifying capacity

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garlic used for

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reduce cholesterol

expectorant

antiseptic

antiviral

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what part of garlic is active

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allicin

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what part of garlic is thought to have antiseptic/viral activity

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sulfur

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single agents/ drugs are ofentimes subsequently synthesized for --- ---- ---- and drug -----

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rigorous biological evaluation

supply

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t/f

secondary metabolites are not absolutely required to sustain life

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t

generally produced for their defense

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single agents/drugs are mainly from

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terrestrial/soil

more recent: marine

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asa is from

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salicyclic acid

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morphine is from

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poppy

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taxol is from

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pacific yew

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vincristine is from

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madagascar periwinkle

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nd derived forma natural produce and is usu a --- modification

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semisynthetic

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how are synthteic drugs found

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usu by random screening/modification of an exidting agent

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biological: usus a large --- or ---- either isolated from an organism/cell line or produced by ---- means ina surrogate host

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peptide

protein

biotechnological

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major issue w/ supply

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natural product is minor extract component

large-scale recollection/fementation impossible

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what's the problem w/ reproducibility

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real producer?: from plant or bacteria

seasona variaein/environmental factors

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prob w/ expense:

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building and maintaining extract collection

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prob w/ time

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tedious isolation

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prob w/ novelty:

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unpredictable

re-isolation of known compound likely

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what's the prob w/ tractability

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sar not straightforward due to structural complexity

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what's the prob w/ intellectual property

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authorization to collect in foreign countries difficult to obtain

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how long can it take for approval of a new drug

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10-15 yrs

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how do you fix the supply issue

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semisynethsis

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which has more chiral centers:

natural products, drugs, synthetics

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np>drugs>synthetics

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what has a higher number of N atoms:

natural products, drugs, synthetics

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synthetics > drugs > np

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which has a higher no of O atoms

natural products, drugs, synthetics

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np>drugs>synthetics

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higher # of rings

natural products, drugs, synthetics

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synthtics>drugs>np

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natural products are prescreened by

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evolutionary selection

produced for self-protection: antifungal/bacterial/viral/feedant

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what are the starting points of drug discovery

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natural products

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characteristics of cocaine:

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3 amine (hydrophilic)

esternyll

carbonyl

lipophilic: aromatic ring. . .can enter membrane

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what has a bunch of acetyl units

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linear acetagonins/polyketides

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１４日

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じゅぅよっか

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alkaloids are basic/acidic

has an -- w/ ---- oxidation sate

hetero----

non common

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basic

N

negative

heterocyclic

not common: not NADH, seotonin

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peptides are ---- made

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nonribosomally made

mainly produced by bacteria and fungi

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what's the greatest reservoir of biological and chemical diversity

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ocean

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1st marine natural product

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conotoxin: zicotidinide

analgesic

100-1000 x potent than morphine

ccb

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2nd marine natural product drug

what's it used for

moa

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cyanosafracin b

refractory advanced tissue sarcoma

effet on transcription-coupled nucleotide excision repair process

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bryostatin used in --- tx

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combo

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bryozoan harbs a --- ---- that may encode biosynthetic genes to produce bryostatin

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symbiotic microorganism

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cryptophycin -52 is under clincial trails

is a synthetic analog of

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cyanobacteria metabolite

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first marine NP in clinical trials as antitumor agent

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didemnin b isolated from tnicate trididemnum

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moa of didemnin b

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binds elongation factor 1 alpha

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ef1 carries aminoacetylated ----- and makes sure it's placed in the ------

also helps w/ recognition of -----

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aminoacetylated

ribosome

codon

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--- was isolated from a slug that feed on cyanobacteria

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dolastatin

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kahalalide f is an --- agent

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antica

isolated from mollusk ( or bacteria)

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halichondrin b and derivatives will be substituted w/ ---- so it's harder to breakdown

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ketone

(so it's more efficacious)

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salinospramide a is an --- agent

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anticancer

produced by a marine derived steptomycete of an entiredly new genus and species

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largazole is a -- selective cytotoxin

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cancer

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largazole is a ---- --- inhibitor

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histone deacetylase inhbitor

(histone removes acetyl from lysine generate a + charge so attracton increases w/ dna - charge)

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how to improve ca tx

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improve tx index of existig drugs

find drugs taht target new proteins/gene products releant to disease

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how do you impove the tx index of existing drugs

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design improved analogues

assur delivery only to target = tumor

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find drugs that target new proteins/gene products?

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find a disease - relevant protein to be inhibited

screen molecules/natural products agaist this target

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targeted delivery using conjuaged -- --- against molecules selectively expressed in ca cells

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monoclonal antibodies

(magic bullet)

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gene expression profiliing is useful in

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finding genes that's overexpressed

this is good for targeting

check rna transcriptase

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ca can be distinguished and grouped by their origin based on --- ---- ---

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gene expression profiles

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ca and the corresponding normal tissues can be distinguished based on their ---- ---

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gene expression

exploit for immunoconjugation of existing drugs or to id novel drug targets

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transcriptiosn is controlled by

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transcription factors

so find gene that control and you can control ca

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--- control signalling in cells

signalling involves transferring ---

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kinases

phosphates

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ca is out of control ----

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signalling

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inhibit ---- ---- this for out of control signalling

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tyrosine kinases

(often overexpressed in ca)

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kinase is an enzyme that binds to --- and transfers --- group onto substrate

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ATP

phosphate

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ser/thr kinases trasner phoshphate onto certain -- and ---- residue of substrate

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Ser

Thr

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-- kinases transfer phosphate onto tyr residue of substrate

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Tyr

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mnay receptors on cell survace have kinase activity

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tyr

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how to inhibit a kinase

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bind to where atp is usu bound

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competitive vs. noncompet

most inhibitors occupy atp binding site

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competitive

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competitive vs. noncompet

allosteric inhibitors

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noncompettive

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which is selectively difficult to achieve

competitive vs. noncompet

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competitive. .. inhibitors occupying atp binding site

although not impossible

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how do you target chronic myeloid leukemia

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target BCR-ABL fusion ogene as a result of reciprocal translocation btw chromosomes 9 and 22

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tyrosine kinase bcr-abl activates multiple --- -----

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signaling pathways

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bcr-abl is --- active

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constitutively

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what do you use against chronic myeloid leukemia

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tyr kinase inhibitor

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-- group reduces activity again another kinase thus increase ---

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methyl

selectivity

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what's overexpressed in 20-30% of invasive breast ca

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HER 2

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how does herceptin target rtk her2

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use an antibody to block kinase

nontoxic

selective antibody

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how do you stop the nf-kb pathway

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use a repressor that makes it stay in the cytoplasm

inhibit the kinase that phosphoylates ikb that release s nkfb and causes translocation into the nucleus

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how do you prevent nk-fb activation

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inhibit kinase

prevent receptor signaling

stabilize endogenous inhibitor

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how do you overcome epigenetic gene silencing

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histone deacetylase inhibitors

prevent deacetylation. . . this reduces the net charge. . .reduces electrostatic interaction btw dna and histones. .. activation of gene expression

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how do you reduce the charge

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change from amine to amide

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an exam of two hdac inhibitors

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saha

fk228

largazole needs approval