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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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Belinostat (PXD101)


File:Belinostat.svg

 

Belinostat (PXD101)

SPECTRUM

Tiny Biotech With Three Cancer Drugs Is More Alluring Takeover Bet Now
Forbes
The drug is one of Spectrum’s two drugs undergoing phase 3 clinical trials. Allergan paid Spectrum $41.5 million and will make additional payments of up to $304 million based on achieving certain milestones. So far, Raj Shrotriya, Spectrum’s chairman, 

http://www.forbes.com/sites/genemarcial/2013/07/14/tiny-biotech-with-three-cancer-drugs-is-more-alluring-takeover-bet-now/

Belinostat (PXD101) is experimental drug candidate under development byTopoTarget for the treatment of hematological malignancies and solid tumors. It is a histone deacetylase inhibitor.[1]

In 2007 preliminary results were released from the Phase II clinical trial of intravenous belinostat in combination with carboplatin and paclitaxel for relapsedovarian cancer.[2] Final results in late 2009 of a phase II trial for T cell lymphomawere encouraging.[3] Belinostat has been granted orphan drug and fast trackdesignation by the FDA.[4]

 

  1.  Plumb, Jane A.; Finn, Paul W.; Williams, Robert J.; Bandara, Morwenna J.; Romero, M. Rosario; Watkins, Claire J.; La Thangue, Nicholas B.; Brown, Robert (2003). “Pharmacodynamic Response and Inhibition of Growth of Human Tumor Xenografts by the Novel Histone Deacetylase Inhibitor PXD101”. Molecular Cancer Therapeutics 2 (8): 721–728. PMID 12939461.
  2.  “CuraGen Corporation (CRGN) and TopoTarget A/S Announce Presentation of Belinostat Clinical Trial Results at AACR-NCI-EORTC International Conference”. October 2007.
  3.  Final Results of a Phase II Trial of Belinostat (PXD101) in Patients with Recurrent or Refractory Peripheral or Cutaneous T-Cell Lymphoma, December 2009
  4.  “Spectrum adds to cancer pipeline with $350M deal.”. February 2010.

SEE COMPILATION ON SIMILAR COMPOUNDS AT …………..http://drugsynthesisint.blogspot.in/p/nostat-series.html

APAZIQUONE


File:Apaziquone.svg

APAZIQUONE

Apaziquone (EOquin[1]) is an indolequinone that is a bioreductive prodrug and a chemical analog of the older chemotherapeutic agent mitomycin C. In hypoxic cells, such as those on the inner surface of the urinary bladder, apaziquone is converted to active metabolites by intracellular reductases. The active metabolites alkylate DNA and lead to apoptotic cell death.[2] This activity is preferentially expressed in neoplastic cells.

Cystoscopic appearance of tumors in the bladder.

After administration of apaziquone directly into the urinary bladder, the drug and its active metabolite were not detected in plasma, and there were no systemic side effects[3][4]

Apaziquone bladder cancer staging

Bladder Cancer

Apaziquone has been applied in clinical studies sponsored by Spectrum Pharmaceuticals and Allergan, Inc. for the treatment of superficial (non-muscle invasive) bladder cancer.[3] Approximately 70% of all newly diagnosed patients with bladder cancer have non-muscle invasive bladder cancer and over one million patients in the United States and Europe are affected by the disease. The US Food and Drug Administration (FDA) has granted Fast Track review status to apaziquone for this indication.[5]

  1.  “UvA researcher develops new bladder cancer medication”. University of Amsterdam. 25 Jul 2007. 

  2. NCI. “apaziquone”. Archived from the original on 9 May 2009. Retrieved 2009-06-07. 
  3. Puri R, Palit V, Loadman PM, et al. (October 2006). “Phase I/II pilot study of intravesical apaziquone (EO9) for superficial bladder cancer”. J. Urol. 176 (4 Pt 1): 1344–8. doi:10.1016/j.juro.2006.06.047. PMID 16952628
  4.  Hendricksen K, Gleason D, Young JM, et al. (July 2008). “Safety and side effects of immediate instillation of apaziquone following transurethral resection in patients with nonmuscle invasive bladder cancer”. J. Urol. 180 (1): 116–20. doi:10.1016/j.juro.2008.03.031. PMID 18485407
  5.  “FDA Designates Fast Track Status For Apaziquone (EOquin) For Bladder Cancer”. Medical News Today. 22 Jul 2009. 

Spectrum Pharmaceuticals  CLICK HERE

Cannabis-Linked Cell Receptor Might Help Prevent Colon Cancer


The study was published in the Aug. 1 issue of the journal Cancer Research.

A cannabinoid receptor lying on the surface of cells may help suppress colorectal cancer, say U.S. researchers. When the receptor is turned off, tumor growth is switched on. Cannabinoids are compounds related to the tetrahydrocannabinol (THC) found in the cannabis plant.

 

It’s already known that the receptor, CB1, plays a role in relieving pain and nausea, elevating mood and stimulating appetite by serving as a docking station for the cannabinoid group of signaling molecules. This study suggests that CB1 may offer a new path for cancer prevention or treatment.

 In the study of human colorectal tumor specimens, the researchers also found that the drug decitabine can restore CB1 expression.In addition, mice those are prone to developing intestinal tumors and also have functioning CB1 receptors developed fewer and smaller tumors when treated with a drug that mimics a cannabinoid receptor ligand, the researchers found. Ligands are molecules that function by binding to specific receptors.

This therapy may help the cancer research team to found out the caner in early stage.

1.     www.washingtonpost.com/wp-dyn/content/article/2008/08/01/AR2008080100937.html

2.      www.medicinenet.com/script/main/art.asp?articlekey=91511

3.      hightimes.com/news/dan/4542    

copy paste link

4.      neurotalk.psychcentral.com/thread51199.html

 
Tetrahydrocannabinol
(−)-(6aR,10aR)-6,6,9-trimethyl-
3-pentyl-6a,7,8,10a-tetrahydro-
6H-benzo[c]chromen-1-ol

Tetrahydrocannabinol (THC), or more precisely its main isomer (−)-trans-Δ9-tetrahydrocannabinol ((6aR,10aR)-delta-9-tetrahydrocannabinol), is the principal psychoactive constituent (or cannabinoid) of the cannabis plant. First isolated in 1964, in its pure form, by Israeli scientists Raphael Mechoulam, Yechiel Gaoni and colleagues at the Hebrew University of Jerusalem, it is a glassy solid when cold, and becomes viscous and sticky if warmed. A pharmaceutical formulation of (−)-trans-Δ9-tetrahydrocannabinol, known by its INN dronabinol, is available by prescription in the U.S. and Canada under the brand name Marinol. An aromatic terpenoid, THC has a very low solubility in water, but good solubility in most organic solvents, specifically lipids and alcohols.

Like most pharmacologically-active secondary metabolites of plants, THC in cannabis is assumed to be involved in self-defense, perhaps against herbivores. THC also possesses high UV-B (280–315 nm) absorption properties, which, it has been speculated, could protect the plant from harmful UV radiation exposure.

Tetrahydrocannabinol with double bond isomers and their stereoisomers is one of only three cannabinoids scheduled by Convention on Psychotropic Substances (the other two are dimethylheptylpyran and parahexyl). Note that cannabis as a plant is scheduled by Single Convention on Narcotic Drugs (Schedule I and IV).

Aiding Computer Aided Drug Design by Shahir shamsir


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Improve Immunity Through Ayurveda


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Greek Herbs- Fennel (saunf)


 
Fennel, otherwise known as Foeniculum vulgare, is a plant belonging to the genus Foeniculum. The fennel plant is native to the Mediterranean region, and the plant produces yellow flowers. Fennel is also an edible plant considered both aromatic and flavorful. In addition to culinary uses, fennel has several purported medicinal uses. Fennel powder is the powdered form made by grinding the seeds from the plant. Health supplement manufacturers use the fennel powder to produce fennel health supplements. You should, however, speak with your doctor prior to using fennel as a health
supplement.

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History of Fennel

Ancient Greeks and Indian cultures used fennel for cooking and as part of traditional herbal medicine. The Greeks and Indians traditionally combined fennel with other herbs to make home remedies for the relief of gastrointestinal problems such as acidity and indigestion.

Fennel Composition

The essential oil of fennel contains approximately 5 percent limonene, 50 to 80 percent anethole and 5 percent fenchone. Additionally, the oil contains trace amounts of a-pinene, estragole, b-pinene, safrole, b-myrcene, camphene and p-cymene. The seeds from the fennel plant also contain fiber and complex carbohydrates. Fennel contains nutrients including vitamin B-3, magnesium, molybdenum, copper, phosphorus, iron, calcium, manganese, vitamin C, folate and potassium.

Fennel Uses

As a health supplement, fennel can help to prevent gas, support digestion and function as an expectorant that can help to relieve minor respiratory problems such as mucus. Fennel also contains anti-inflammatory properties when used externally. The leaves from the fennel plant can facilitate the healing of wounds and burns. The root of the fennel plant is diuretic and can help treat urine infections. Fennel also contains a combination of phytonutrients including the flavonoids rutin, quercitin and kaempferol. Fennel also has antioxidant properties and as a dietary fiber, it can help lower your cholesterol levels.

Fennel Supplements

Health supplement manufacturers offer fennel supplements in powdered form. As a supplement, manufacturers recommend taking 1 to 4 g per day of the powdered fennel supplement. The Food and Drug Administration, however, has not established a recommended dose for fennel powder. There are no known side effects of consuming fennel powder supplements, although you should speak with your doctor prior to using fennel powder if you are attempting to treat a specific medical condition.

The bulb, foliage, and seeds of the fennel plant are widely used in many of the culinary traditions of the world. The small flowers of wild fennel (mistakenly known in America as fennel “pollen” ) are the most potent form of fennel, but also the most expensive.Dried fennel seed is an aromatic, anise-flavoured spice, brown or green in colour when fresh, slowly turning a dull grey as the seed ages. For cooking, green seeds are optimal. The leaves are delicately flavoured and similar in shape to those of dill. The bulb is a crisp vegetable that can be sautéed, stewed, braised, grilled, or eaten raw. They are used for garnishes and to add flavor to salads. They are also added to sauces and served with pudding. The leaves used in soups and fish sauce and sometimes eaten raw as salad.

Fennel seeds are sometimes confused with those of anise, which are similar in taste and appearance, though smaller. Fennel is also used as a flavouring in some natural toothpastes. The seeds are used in cookery and sweet desserts.

Many cultures in India, Pakistan, Afghanistan, Iran and the Middle East use fennel seed in their cookery. It is one of the most important spices in Kashmiri Pandit and Gujarati cooking. It is an essential ingredient of the Assamese/Bengali/Oriya spice mixture panch phoron and in Chinese five-spice powders. In many parts of India and Pakistan, roasted fennel seeds are consumed as mukhwas, an after-meal digestive and breath freshener. Fennel leaves are used as leafy green vegetables either by themselves or mixed with other vegetables, cooked to be served and consumed as part of a meal, in some parts of India. In Syria and Lebanon, it is used to make a special kind of egg omelette (along with onions, and flour) called ijjeh.

Many egg, fish, and other dishes employ fresh or dried fennel leaves. Florence fennel is a key ingredient in some Italian and German salads, often tossed with chicory and avocado, or it can be braised and served as a warm side dish. It may be blanched or marinated, or cooked in risotto.

In Spain the stems of the fennel plant are used in the preparation of pickled eggplants, “berenjenas de Almagro”.

Medicinal uses

Fennel (Foeniculum vulgare) essential oil in clear glass vial

Fennel contains anethole, which can explain some of its medical effects: It, or its polymers, act as phytoestrogens.

The essence of fennel can be used as a safe and effective herbal drug for primary dysmenorrhea, but could have lower potency than mefenamic acid at the current study level.

Intestinal tract

Fennel is widely employed as a carminative, both in humans and in veterinary medicine (e.g., dogs), to treat flatulence by encouraging the expulsion of intestinal gas. Anethole is responsible for the carminative action.

Mrs. Eencher Herbal states:

On account of its carminative properties, fennel is chiefly used medicinally with purgatives to allay their side effects, and for this purpose forms one of the ingredients of the well-known compound liquorice powder. Fennel water has properties similar to those of anise and dill water: mixed with sodium bicarbonate and syrup, these waters constitute the domestic ‘gripe water‘ used to correct the flatulence of infants. Volatile oil of fennel has these properties in concentration. Commercial preparations of fennel  are widely available as alternative treatment for baby colic. Fennel tea, also employed as a carminative, is made by pouring boiling water on a teaspoonful of bruised fennel seeds.

Fennel can be made into a syrup to treat babies with colic (formerly thought to be due to digestive upset), but long-term ingestion of fennel preparations by babies is a known cause of thelarche.

Eyes

In the Indian subcontinent, fennel seeds are also eaten raw, sometimes with some sweetener, as they are said to improve eyesight. Ancient Romans regarded fennel as the herb of sight.Root extracts were often used in tonics to clear cloudy eyes. Extracts of fennel seed have been shown in animal studies to have a potential use in the treatment of glaucoma.

Blood and urine

Fennel may be an effective diuretic and a potential drug for treatment of hypertension.

Breastmilk

There are historical anecdotes that fennel is a galactagogue,improving the milk supply of a breastfeeding mother. This use, although not supported by direct evidence, is sometimes justified by the fact that fennel is a source of phytoestrogens, which promote growth of breast tissue. However, normal lactation does not involve growth of breast tissue. A single case report of fennel tea ingested by a breastfeeding mother resulted in neurotoxicity for the newborn child.

Other uses

Syrup prepared from fennel juice was formerly given for chronic coughs. It is one of the plants which is said to be disliked by fleas, and powdered fennel has the effect of driving away fleas from kennels and stables.

References

  • “Herbs That Work: The Scientific Evidence of Their Healing Powers”; David Armstrong
  • “The Encyclopedia of Herbs: A Comprehensive Reference to Herbs of Flavor and Fragrance”; Arthur O. Tucker and Thomas DeBaggio; 2009
  • “Pocket Guide to Herbal Remedies”; Lane P. Johnson; 2002
  • “Encyclopedia of Natural Medicine”; Michael Murray and Joseph Pizzorno; 1997

seeds

Study links vitamin D deficiency to accelerated bone aging


Robert Ritchie (left) and Hrishikesh Bale used a combination of FTIR spectroscopy and X-ray CT at the Advanced Light Source to find that vitamin D deficiency speeds the aging process of bone and reduces its quality. Photo by Roy Kaltschmidt

Robert Ritchie (left) and Hrishikesh Bale used a combination of FTIR spectroscopy and X-ray CT at the Advanced Light Source to find that vitamin D deficiency speeds the aging process of bone and reduces its quality. Photo by Roy Kaltschmidt

 

A team of scientists led by researchers at Lawrence Berkeley National Laboratory and the Univ. of California, Berkeley, have recently used a combination of Fourier transform infrared spectroscopy and X-ray computed tomography at the Advanced Light Source to find that vitamin D deficiency speeds the aging process of bone and reduces its quality.FULL STORY

http://www.rdmag.com/news/2013/07/study-links-vitamin-d-deficiency-accelerated-bone-aging?et_cid=3362718&et_rid=523036890&type=cta

DRUG DISCOVERY PRESENTATION BY DR ANTHONY CRASTO


 

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Novartis teams with India’s Biological E for typhoid vaccine development


Novartis teams with India’s Biological E for typhoid vaccine…

 

Novartis and Indian biopharma Biological E have entered into a development and licensing agreement  to deliver accessible and affordable typhoid and paratyphoid A vaccines to the developing world. Yearly, over 21 million cases and 5 million cases of typhoid and paratyphoid A… read more ›

read all at

http://blogs.terrapinn.com/vaccinenation/2013/07/10/novartis-teams-indias-biological-typhoid-vaccine-development/?pk_campaign=Blog_Newsletter_Vaccine%20Nation&pk_kwd=2013-07-10&elq=f2955f5ac0f942289fabfdbbde71072c&elqCampaignId=4765&pk_campaign=Blog_Newsletter_Vaccine%20Nation&pk_kwd=2013-07-10&elq=f2955f5ac0f942289fabfdbbde71072c&elqCampaignId=4765

H7N9 vaccines in development–where are we?


influenza h7n9 vaccine development (Photo Credit: CDC/Cynthia S. Goldsmith and Thomas Rowe)

Since early 2013, the newly emergent H7N9 avian influenza virus has been infecting humans in China, leading to the temporary closure of numerous poultry markets in a bid to control the outbreak. In recent weeks, the rate at which new cases are reported has been declining – but some experts are asking whether this is just the calm before the storm. The development of a vaccine against the virus is therefore still of great interest – but where are we with vaccine development?

Inovio Pharmaceuticals announced on July 8th that in a preclinical study of its influenza DNA vaccine, 100% of the vaccinated animals were protected against sickness and death when challenged with a lethal dose of A/Anhui/1/13 strain of H7N9 virus. On the same day, Novavax made an announcement that enrolment had begun for a Phase I clinical trial of its monovalent virus-like particle (VLP) vaccine candidate – again based on the A/Anhui/1/13 strain

read all at

http://blogs.terrapinn.com/vaccinenation/2013/07/09/h7n9-vaccines-developmentwhere/?pk_campaign=Blog_Newsletter_Vaccine%20Nation&pk_kwd=2013-07-10&elq=f2955f5ac0f942289fabfdbbde71072c&elqCampaignId=4765&pk_campaign=Blog_Newsletter_Vaccine%20Nation&pk_kwd=2013-07-10&elq=f2955f5ac0f942289fabfdbbde71072c&elqCampaignId=4765