Dr. Vedamurthy M Bhusainahalli, Research Associate.

Inorganic & Physical Chemistry Department,

Indian institute of Science Bangalore -560012, India.

Phone: +91 -944-***-****, : ab83np@r.postjobfree.com

Personal Information

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Date of Birth: 10 May, 1982.

Nationality: Indian

Marital Status: Unmarried

Permanent Address: Neethigere (p), Channagiri (t), Davangere (d), Karnataka (s), India -577215

Education

Indian Institute of Science Bangalore, India

Research Associate, May 2012-Present.

University of Catania

Department of Chemical Sciences Catania, Sicily, Italy

PhD (Organic Chemistry), Nov 2008- March 2012.

Institute of Molecular Chemistry at the University Dijon, France

of Burgundy, Part of Ph.D work, Feb 2011-March 2011.

Jawaharlal Nehru Centre for Advanced Scientific Research Bangalore, India

Pre-doctoral fellow (R&D Assistant, Organic Chemist)

Molecular Biology and Genetics Unit, Feb 2006-Oct 2008.

Kuvempu University Karnataka, India

Master of Science in Industrial Chemistry,

School of Chemical Sciences, 2003- 2005.

Research Experience

Postdoctoral work Title: Development of selenium based drugs as novel anti -cancer agents targeting the

immune regulatory enzymes. (May 2012-Present)

Advisor: Prof. G Mugesh

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The synthesis of peptides containing selenocysteine (Sec) is rapidly gaining interest with the discovery of an

increasing number of proteins containing amino acid. In addition, selenocysteine derivatives can serve as

convenient precursors to dehydroamino acids, which are useful electrophilic handles for the chemoselective

preparation of peptide conjugates. Importantly, selenium is an essential trace element for mammals, and

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selenocysteine was established as the 21 proteinogenic amino acid. Fmoc-protected amino acids have been

used as precursors for solid-phase peptide synthesis (SPPS) of selenocysteine-containing peptides. An objective

of this work is to design, synthesis and characterization of peptides containing selenocysteine and study of

enzymatic deiodination of thyroxine by the synthesized selenocysteine -containing peptides.

Ph.D. Thesis Title: Natural polyphenols as lead compounds in the synthesis of antitumor agents and other

useful products. (Nov 2008- March 2012)

Advisor: Prof. Corrado Tringali

We have investigated the oxidative coupling of some simple analogues of natural polyphenols. In the case of

stilbenolignans, the monomeric stilbenoids were prepared through Wittig-like and/or Heck reactions.

Synthetic viniferins were obtained from monomers through a coupling reaction mediated by metal and/or

enzymes such Horseradish peroxidase and/or laccase from Trametes versicolor. In these reactions after the

formal removal of a hydrogen atom from the p-phenolic group a phenoxy radical with the unpaired electron at

the C-β position may couple with another C-5 radical (β-5’ coupling) to generate a reactive bis-

quinonemethide; the subsequent intramolecular cyclization and aromatization lead to the final product. Due

to the lack of stereocontrol both in metal and enzyme mediated phenolic radical coupling, racemic mixtures

are frequently obtained. Racemic mixtures and pure enantiomers were subjected to antiproliferative activity

towards SW480 colon cancer cell lines. Our results suggest that only S enantiomers were more active than R

enantiomers and Resveratrol and Viniferin used as control ( EJOC, Volume 2012, Issue 27, pages 5217–5224,

September 2012).

On the basis of a similar methodology, α,β-unsaturated carboxylic amides (p-coumaric, caffeic and ferulic

amides) were subjected to both chemical- or enzyme-mediated oxidative coupling reactions. Employing

Laccase from Pleurotus ostreatus, nitrogenated dihydrobenzofuran neolignans (lignanamides), were obtained.

By using manganese triacetate on the caffeic amide, a new fluorescent benzo[kl]xanthene lignanamide was

obtained. These dimers are strictly related to neolign ans and benzoxanthene lignans previously reported as

antiangiogenic, antiproliferative and DNA-interacting agents. (Published in proceedings: XXXIV Convegno

Nazionale Divisione Di Chimica Organica, held at Pavia, Italy)

On behalf of our main project, we have obtained as unexpected products caffeoyl N-acylureas, which were

subjected to enzyme-assisted reactions yielding hydantoin derivatives in very mild conditions. We have

systematically studied the reaction mechanism of hydantoins by using symmetric and asymmetric

carbodiimides; a detailed study of the influence of key reaction parameters such as solvent, enzyme, metal

mediated salts and structure of the reactants on the reaction outcome and mechanism has been carried out

and will be presented in a forthcoming Symposium. (Manuscript submitted to Organic Letter).

Pre-doctoral research: Small molecule modulators of histone modifying enzymes and chromatin therapy.

(Feb 2006-Oct 2008)

Advisor: Prof. Tapas Kumar Kundu

Small molecule inhibitors and activators of HATs are being considered as new generation therapeutics In view

of this, we synthesized specific and less toxic inhibitors/activators of HATs (from garcinol, isogarcinol and

curcumin) by isolating and semisynthesis of the compounds from natural sources. And then, we studied the

mechanistic aspect of inhibition/activation in great detail which could be useful for future rational drug

designing. (Chem. Biol. 17(8):903-13 and J Med Chem. 2009 Jan 22; 52 (2):267-77).

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There are three classes of aurora kinases in humans: A, B, and C. Aurora kinase A is frequently overexpressed

in various cancers. By employing virtual screening, we have found that anacardic acid, a pentadecane aliphatic

chain containing hydroxylcarboxylic acid and its analogues, from cashew nut shell liquid could be doc ked in

Aurora kinases A and B. Remarkably, we found that anacardic acid could potently activate the Aurora kinase A

mediated phosphorylation of histone H3, but at a similar concentration the activity of aurora kinase B

remained unaffected in vitro. (J Med Chem. 2008 Feb 28;51(4):792-7).

Scientific Publications

A. Hari Kishore, B.M.Vedamurthy, K.Mantelingu, Shipra Agarwal, B. A. Ashok Reddy,Siddhartha Roy,

Rangappa K. S and Tapas K. Kundu. (2008) Specific small molecule activator of Aurora Kinase A

Induces Autophosphorylation in a cell free system. J Med Chem. 2008 Feb 28;51(4):792-7.

Arif M, Suman Kalyan Pradhan, Thanuja G R, B.M.Vedamurthy, Mantelingu K, Dipak Dasgupta and

Tapas K Kundu. (2008). Mechanism of p300 Specific Histone Acetyltransferase Inhibition by Small

Molecules. J Med Chem. 2009 Jan 22;52(2):267-77.

Arif M, Vedamurthy M. Bhusainahalli, Choudhari R, Ostwal YB, Mantelingu K, Kodaganur GS, Kundu

TK. (2010). Nitric oxide-mediated histone hyperacetylation in oral cancer: target for a wat er-soluble

HAT inhibitor, CTK7A. Chem Biol. 17(8):903-13.

Vedamurthy M. Bhusainahalli, M. Chalal, C. Spatafora, D. Vervandier-Fasseur, Philippe Meunier N.

Latruffe, C. Tringali. Resveratrol-Related Dehydrodimers: Laccase-Mediated Biomimetic Synthesis and

Antiproliferative Activity. European Journal of Organic Chemistry, Volume 2012, Issue 27, pages

5217–5224, September 2012.

Snehajyoti Chatterjee, Pushpak Mizar, Raphaelle Cassel, Romain Neidl, B. Ruthrotha Selvi, DV

Mohankrishna, Bhusainahalli M Vedamurthy, Anne Schneider, Olivier Bousiges, Chantal Mathis, Jean -

Christophe Cassel, M Eswaramoorthy, Tapas Kundu, and Anne-Laurence Boutillier Brain-targeted

small molecule activator of CBP/p300 acetyltransferases promotes neurogenesis and extends memory

duration in adult mice.(Manuscript submitted to Journal of Neuroscience)

Vedamurthy M. Bhusainahalli, C. Spatafora, A. Rescifina, U. Chiacchio, C. Tringali. Laccase enzyme-

assisted ‘green’ synthesis and mechanistic study of new hydantoin derivatives.(Manuscript submitted

to Organic Letter)

Vedamurthy M. Bhusainahalli, C. Spatafora, and C. Tringali. (2012) Bio-inspired benzo[kl]xanthene

lignans: design, synthesis, DNA-interaction and antiproliferative properties.(Manuscript in

preparation)

Patent:

Title of the Invention: Histone Acetyltransferase (HAT) Activator Composition and Process Thereof.

Inventors: Kundu T. K., Boutillier A.L., Chatterjee S., Eswarmoorthy M., Mizar P., Mathis C., Cassel J.

C., Neidl R., D. V. Mohankrishna., Vedamurthy B. M.

Indian Provisional Patent Application No. 4646/CHE/2011

Proceedings in Conferences

Carmela. Spatafora, Vedamurthy M. Bhusainahalli, Malik. Chalal, Dominique. Vervandier-Fasseur,

Noberet. Latruffe, C. Tringali, Resveratrol-Related Dehydrodimers: Laccase-Mediated Biomimetic

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Synthesis and Antiproliferative Activity. XXVI International Conference on Polyphenols. Florence,

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Italy, 23 -26 July 2012. Polyphenols Communications- 2012, Volume 1/O.29, p-88

Carmela Spatafora, Vedamurthy Bhusainahalli, Simone Di Micco, Nicolò Musso, Raffaele Riccio,

Giuseppe Bifulco, Daniele Condorelli, Corrado Tringali. “Bio-inspired benzo[kl]xanthene lignans:

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design, synthesis, DNA-interaction and antiproliferative properties”. XXXIV Convegno Nazionale

Divisione Di Chimica Organica, Pavia, Italy 10-14 settembre 2012, OC-48, P-81.

Oral communication in Conferences

V.M. Bhusainahalli, M. Chalal, C. Spatafora, D. Vervandier-Fasseur, N. Latruffe, C. Tringali (2010).

Biomimetic Synthesis of Stilbenolignans and their antiproliferative Activity towards colon cancer cells.

In: Joint Meeting of Italian Chemical Society - Sections Calabria and Sicily. Palermo, 2-3 December

2010 - p. O13.

V.M. Bhusainahalli, C. Spatafora. C, Tringali C (2009). Biomimetic Synthesis of lignans and related

products from natural polyphenols. In: Joint Meeting of Italian Chemical Society - Sections Calabria

and Sicily Aci Castello (Catania) 1-2 December 2009 - p. O16.

Poster presentation in Conferences

V.M. Bhusainahalli, M Arf, Suman Kalyan Pradhan, Thanuja G R, Mantelingu K, Dipak Dasgupta and

Tapas K Kundu. (2009). Mechanism of p300 Specific Histone Acetyltransferase Inhibition by Small

Molecules. In: Proceedings of the VIII National Congress of Chemistry of Natural Substances Forte dei

Marmi, 22-25, May 2009 - p. P3.

V.M. Bhusainahalli, C. Spatafora, M. Chalal, C. Spatafora, D. Vervandier -Fasseur, N. Latruffe, C.

Tringali. (2011) ‘Unnatural’ viniferins: Biomimetic synthesis and antiproliferative activity. In:

NatPharma: Nature Aided Drug Discovery. Napoli, 5-9 June, 2011- p. P24

Conferences attended

Asian Chromatin Forum First meeting of Chromosome and Chromatin Biology, Decembe r 11-13, 2006

at JNCASR, Bangalore, India

NCBS-JNCASR-Harvard Symposium on “Interdisciplinary Materials Science, Computation and Biology”

held at JNCASR/NCBS from August 11-13, 2006

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ACS in India held at Indian Institute of Science, Bangalore, India. on Oc tober 3 2012

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6 International Meeting on Halogen Chemistry (HALCHEM-VI) held at Department of Inorganic &

Physical Chemistry, Indian Institute of Science, Bangalore, India -12. On December 8-11 2012

Technical Experience

Organic Chemistry:

Reactions carried out: in inert atmosphere (for C -C bond formation), in Hydrogen atmosphere

(reduction of C-C double bond), Oxidation reactions in atmospheric oxygen (radical coupling

reactions), C-Li, C-Se, and Se-N bond formation reactions, amidation, esterification, alkylation,

acyltion, diazotization reaction etc.

Hands in enzymatic reactions, Green chemistry (eco -friendly reactions), Use of metal inorganic salts in

organic reactions, Use of coupling reagents, Use of oxidation and reduction reagents etc.

Extensive experience with Schlenk-line techniques and air-free synthetic methods.

Experience in extraction and isolation of plant materials like Garcinia indica, Curcuma longa,

Plumbago rosea, and Anacardiaceae.

Well versed in recrystallization, separation, purification, drying, and identification techniques.

Practical and IT Skills:

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NMR: Handling of Bruker 400 MHz NMR spectrometers, H, C, Se and analysis of HSQC, HMBC,

COSY,1D-Noesy. software: Xwinnmr, Topspin. Handling of ESI-Mass spectrometer.

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Handling of HPLC (Agilent 1100 auto sampling) analytical and chiral column, Biotage Flash-

Chromatography (medium pressure), Column Chromatography, lyophilizer, Catalytic hydrogenation

instrument for reduction of alkenes.

Experience in the supervision of undergraduate students research projects.

Software: Office software, SciFinder, Scopus, Scirus, Chemdraw, ACD Chem sketch C-H analyzer,

Chem spider, e-molecule, pub-med molecule, Photoshop.

References

Dr. Corrado Tringali, Full Professor, Ph.D Supervisor

Dipartimento Scienze Chimiche, University di Catania, V.le Andea Doria 6, I-95125, Catania, ITALY.

tel :+390**-*******, E-mail: ab83np@r.postjobfree.com

Dr. Carmela Spatafora, Assistant Professor, Co-guide

Dipartimento Scienze Chimiche, University di Catania, V.le Andea Doria 6, I-95125, Catania, ITALY.

tel :+390**-*******,E-mail: ab83np@r.postjobfree.com

Dr. K Mantelingu, Assistant Professor, Pre-Ph.D Co-guide

Department of Chemistry, University of Mysore, Mysore -57006, India.

tel:+91-974*******, E-mail: ab83np@r.postjobfree.com

(Vedamurthy BM.)

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