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NEWS LETTERS
BIOCHEMICAL AND PHARMACOLOGICAL ACTIVITY OF FLAVONES, ISOFLAVONES, COUMARINS , CHALKONES AND CHROMONES.
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FLAVONIODS ARE 
UBIQUITOUS IN
FLOWERING 
PLANTS

 

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The above ring systems were reported to display a wide variety of biochemical and pharmacological activities as reported in various research journals during the period 1990-2000.

Recent  Advances (1991-2000)

--- Potent and Specific inhibition of cAMP phosphodiesterase.
--- Protein Kinase C activity.
--- Antineoplastic agents (many flavones reported to have this 
     activity) activity against pancreatic cancer.
---- to treat inflammation (anti-inflammatory activity) and arthiritic 
     conditions.
---- Antiallergic and  antiasthmatic agents (several chromones were 
      reported to have this activity)
--- 5 – Lipoxygenase inhibitors.
--- Cyclooxygenase inhibitors.
--- Agents for the treatment of osteoporosis.
--- Potent antithrombotic agents.
--- Potent, selective, non-cytotoxic inhibitor of 
     phosphatidylinositol-3-Kinase.
--- Immunomodulator agent.
--- Potent bone resorption inhibitor that activates protein kinase C 
     activity.
--- Potent uroselective alpha-1-adrenoceptor antagonist with additional 
     5-HTIA receptor – antagonist activity.
--- Platelet antiaggregatory agents.
--- Antiestrogenic, antineoplastic agents (with topoisomerase- 
      I inhibitory activity).
--- Antibacterial agents.
--- Antiproliferative agents.
--- Antitumor and antimetastic agents.
--- Cardioprotective agents with potent antiplatelet activity.
--- Disodium chromoglycate (chromone derivative) is a commercial drug 
     as an antiallergic agent to treat asthma.
--- Symptomatic antidiabetic agents, aldose reductase inhibitor.
--- Dopamine autoreceptor agonist.
--- Leukotriene B4-antagonist.
--- Cardioprotective agents.
--- Antipsychotic and neuroprotective agents.
--- Antidepressant agents.
--- Anticonvulsant and neuroprotective agents.
--- Antidementia agents (coumarins especially)
--- Agents to treat atherosclerosis.
--- to treat AIDS,  Anti-HIV agents.  Some natural coumarins are potent 
    and selective non-nucleoside HIV – 1 reverse transcriptase inhibitors.
---Coronary vasodilating and antihypertensive agents (coumarins 
    especially)
--- Antiviral agents.
--- Selective dopomine autoreceptor agonist.
--- Thromboxane A2 (TxA2) synthatase – inhibitory activity.
--- Antimalarial agent that inhibits that inhibits the growth of both 
     chloroquine-sensitive (D6) and multidrug-resistant (W2) strains of 
     Plasmodium faclciparum in vitro (xanthones especially)
--- Agents to treat atherosclerosis and mycocardial ischemia (coumarins 
     especially)
--- Anticonvulsant and neuroprotective agents (Coumarins especially)
--- Agents to treat cerebrovascular disorders.
--- Antidepressants.
--- Potentially useful for improving circulatory system, kidney functions 
    and treating stress.
--- Hypotensive induced Ulcers.
--- To treat psoriasis and Vitilago.
--- Urinary disorders ( A commercial drug, flavoxate, for example).
--- Antioxidants ( A number of flavones which have ortho-dihydro 
     system, for example quercetin, (-) -epi-catechin, procyanidin 
     isomers,anthocyanins,red wine,green tea extract,grape seed extract 
     and pine bark extract which contain flavonoids,catechins and 
     procyanidin are excellent antioxidants. These are available 
     Commercially).

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--- Phytoestrogens (Isoflavones like genistein, daidzein found in soy 
     beans.  These isoflavones have antioxidant activity also. Coumestans
     also have phytoestrogenic activity).
---Flavonoids found in plants involve protection of plants  against pests 
    ,virus,bacteria and fungi, attraction of pollination , promotes   fertility 
    and germinination and as oviposition stimulants .Infact flavonoids act 
    as defensive agents--phytoalexins, alleopathic and insect-antifeedant 
    agents-- to protect the plants.
--- The role of  natural  flavonoids as  antiviral , antifungal ,in human 
     medicine is well recorded.
--- Recent studies revealed that food beverages (wine,beer,green tea) 
    fruits and vegetables and honey  are known to have antioxidant
     activity
---In general plant phenolics including catechins and procyanidins are 
    antioxidants , known to possess anicarcinogenic,antiallergic and 
    anti-inflammatory properties.
---Centochroman (chroman derivative, contraceptive agent),silibyn 
    (natural flavonoid,hepato protective agent), flavoxate hydrochloride 
    (flavone derivative,diuretic agent),rotenone (natural isoflavanone 
    derivative,insecticidal),Disodium chromoglycate
    (chromone derivative,antiallergic agent to treat
     asthma),psoralen,trimethylpsoralen 
    and methoxalen (furanocoumarins,to treat vitiligo ,leucoderma and 
    psoriasis),dicoumarol(coumarin derivative, blood anticoagulating 
    agent) are commercially available. 
---Several chromones,flavones and coumarins are in various stages of 
    clinical trials as drugs. 

The Literature Survey is based on reports from:
--- Annual drug data report.
--- Drug data report.
--- Drugs for future.
--- Journal of medicinal chemistry and other journals and patent search.
--- Annual reports in medicinal chemistry.
---Monographs  on natural products

Based on the study, the  Synthesis and biological screening of chromones, flavonoids, coumarins,isoflavones and chalkones etc.with subsituents at various positions will be rewarding.A new range of products included in our synthetic programme are several substituted derivatives  of these oxygen heterocycles .
 
 

 

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