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Dr. Amit Shard, Ph.D.

Assistant Professor , Department of Medicinal Chemistry

Research Interest

(i) Development of novel PKM2 modulators.
(ii) Design, synthesis, computational validation of hetero (aromatic) molecules with drug like properties.
(iii) In area of cancer, our group is focusing on finding potential lead molecules against tumor M2 Pyruvate Kinase (M2PK) enzyme having widespread occurrence in several cancer types.

Experience

  • June 2014-Present
    Assistant Professor

    NIPER-Ahmedabad, Palaj Gandhinagar

  • April, 2011-April 2014
    Senior Research Fellowship

    by Council of Scientific and Industrial Research, New Delhi

  • July 2008-March 2011
    Project Assistantship

    CSIR-IHBT, Palampur, H.P

Honours

  • Young Achiever Award-2016, by SBSOSA, S.B.S. P.G.I, Dehradoon.
  • Recent work published in European Journal of Organic Chemistry (2016) was highlighted in the form ofvideoby the journal. The work was considered highly significant.
  • Central Drug Research Institute awarded CDRI-Research Incentive Award -2016.
  • Best poster award- 2013 on at B.H.U Varanasi in conference organized by Chemical Research society (CRSI) of India.
  • Award by the Institute of Himalayan Bioresource Technology, Palampur on national science day (28th of Feb) for publishing an article in Angew. Chem. Int. Edn (2013)..
  • Dr. P. D. Sethi annual award-2012 for best research paper (Angew. Chem. Int. Edn. 2012, 51, 2636-39) on Application of HPTLC in Pharma, Herbal and other Chemical Analysis.
  • Award by the Institute of Himalayan Bioresource Technology, Palampur on National Science Day (28th of Feb) for publishing an article in Angew. Chem. Int. Edn (2012).
  • Best poster award at CRSI North Zone meeting, at Jammu University (2011).

Publications

1. Kumar, S. P., Jadav, T., Sahu, A. K., Ghosh Chowdhary, M., Siwach, A., Patel, H., Patel, S., Rajput, N., Shard, A., Khairnar, A., & Sengupta, P. (2023). Assessment of metabolic stability and pharmacokinetics by LC–MS/MS and establishment of the safe dose of IMID-2, a novel anticancer molecule under drug discovery. Biomedical Chromatography, e5618. https://doi.org/10.1002/bmc.5618
2. Kapoor, Amit Shard Roadmap to Pyruvate Kinase M2 Modulation – A Computational Chronicle” Just accepted “Current Drug Targets”
3. Tambe, V., Patel, S., Shard, A., Behera, S.K., Polaka, S., Anup, N., Gadeval, A., Kalia, K. and Tekade, R.K., 2022. Dendronized Polymeric Biomaterial for Loading, Stabilization, and Targeted Cytosolic Delivery of microRNA in Cancer Cells. ACS Applied Bio Materials. Impact Factor (3.25)
4. Chatterjee, D.R., Kapoor, S., Jain, M., Das, R., Chowdhury, M.G. and Shard, A., 2022. PROTACting the kinome with covalent warheads. Drug Discovery Today, p.103417. Impact Factor (8.3)
5. Chowdhury, M.G., Das, R., Vyas, H., Sasane, T., Mori, O., Kamble, S., Patel, S. and Shard, A., 2022. A Comprehensive Account of Synthesis and Biological Activities of α‐lidene‐Benzocycloalkanones and Benzoheterocycles. ChemistrySelect, 7(33), p.e 202201468. Impact Factor (2.3)
6. Gupta, Astha, Rudradip Das, Ambika Chamoli, AsmitaChoithramani, Hansal Kumar, Sagarkumar Patel, Shard, A., 2022. “A Series of Ferrocene-Containing Pyrazolo [1, 5-a] pyrimidines Induce a Strong Antiproliferative Effect against Oral Cancer Cells.” Organometallics, 41(16), 2365-2378. Impact Factor (3.8)
7. Jadhav, J., Das, R., Gupta, A., Shard, A. 2022. Ferrocene-Based Modulators of Cancer-Associated Tumor Pyruvate Kinase M2″ Journal of Organometallic Chemistry, 968. Impact Factor (2.36)
8. Das, R., Kapoor, S. & Shard, A. 2022. Docking, ADMET and Molecular Dynamics Studies of Natural Polyphenolics as Tumor Pyruvate Kinase M2 Modulators. Indian Forester, 148(4), 368-380. Impact Factor (0.66)
9. Rihan M, Vineela Nalla L, Dharavath A, Patel S, Shard A, Khairnar A. 2022. Boronic acid derivative activates pyruvate kinase M2 indispensable for redox metabolism in oral cancer cells. Bioorg Med Chem Lett. 1;59:128539. Impact Factor (2.82)
10. Das, R., Choithramani, A., & Shard, A. 2021. A molecular perspective for the use of type IV tyrosine kinase inhibitors as anticancer therapeutics. Drug Discovery Today, 27(3), 808-821. Impact Factor (8.3)
11. Patel, S., Globisch, C., Pulugu, P., Kumar, P., Jain, A., & Shard, A. 2022. Novel imidazopyrimidines-based molecules induce tetramerization of tumor pyruvate kinase M2 and exhibit potent antiproliferative profile. European Journal of Pharmaceutical Sciences, 170, 106112. Impact Factor (4.379)
12. Das, R., Chowdhury, M. G., Raundal, S., Jadhav, J., Kumar, N., Patel, S., & Shard, A. 2022. Objective Assessment of Adrenocortical Carcinoma Driver Genes and Their Correlation with Tumor Pyruvate Kinase M2. Gene, 146354. Impact Factor (3.8)
13. Rathod, B., Chak, S., Patel, S., & Shard, A. 2021. Tumor pyruvate kinase M2 modulators: a comprehensive account of activators and inhibitors as anticancer agents. RSC Medicinal Chemistry. Impact Factor (3.47)
14. Behera, S. K., Vhora, N., Contractor, D., Shard, A., Kumar, D., Kalia, K., & Jain, A. 2021. Computational drug repurposing study elucidating simultaneous inhibition of entry and replication of novel corona virus by Grazoprevir. Scientific reports, 11(1), 1-11. Impact Factor (4.379)
15. Panday, N. K., Thakkar, D., Patel, S., Shard, A., & Sengupta, P. 2021. Metabolite profiling of IMID‐2, a novel anticancer molecule of piperazine derivative: In silico prediction, in vitro and in vivo metabolite characterization using UPLC–QTOF–MS/MS. Biomedical Chromatography, 35(6), e5082. Impact Factor (1.902)
16. Patle, R., Shinde, S., Patel, S., Maheshwari, R., Jariyal, H., Srivastava, A., & Shard, A. 2021. Discovery of boronic acid-based potent activators of tumor pyruvate kinase M2 and development of gastroretentive nanoformulation for oral dosing. Bioorganic & medicinal chemistry letters, 42, 128062. Impact Factor (3.641)
17. Patel, S., Das, A., Meshram, P., Sharma, A., Chowdhury, A., Jariyal, H., …& Shard, A. 2021. Pyruvate kinase M2 in chronic inflammations: a potpourri of crucial protein–protein interactions. Cell Biology and Toxicology, 1-26. Impact Factor (6.691)
18. Bhute, S., Sarmah, D., Datta, A., Rane, P., Shard, A.,Goswami, A., & Bhattacharya, P. 2020. Molecular pathogenesis and interventional strategies for Alzheimer’s disease: promises and pitfalls. ACS pharmacology & translational science, 3(3), 472-488.
19. Zagade, A. D., Shard, A., Shinde, S., Sahu, A. K., & Sengupta, P. 2020. Bioanalysis and Quadrupole-Time of Flight-Mass Spectrometry Driven In Vitro Metabolite Profiling of a New Boronic Acid-Based Anticancer Molecule. Journal of Chromatographic Science, 58(9), 796-803. Impact Factor (1.618)
20. Chowdhury, A., Patel, S., Sharma, A., Das, A., Meshram, P., & Shard, A. 2020. A perspective on environmentally benign protocols of thiazole synthesis. Chemistry of Heterocyclic Compounds, 56(4), 455-463. Impact Factor (1.277)
21. Sahu, B., Behera, S. K., Das, R., Dalvi, T., Chowdhury, A., Dewangan, B., …& Shard, A. 2020. Design and in-silico screening of Peptide Nucleic Acid (PNA) inspired novel pronucleotide scaffolds targeting COVID-19. Current Computer-aided Drug Design. Impact Factor (1.606)
22. Madasu, J., Shinde, S., Das, R., Patel, S., & Shard, A. (2020). Potassium tert-butoxide mediated C–C, C–N, C–O and C–S bond forming reactions. Organic & Biomolecular Chemistry, 18(41), 8346-8365. Impact Factor (3.876)
23. Patel, S., Rathod, B., Regu, S., Chak, S., & Shard, A. (2020). A Perspective on Synthesis and Applications of Fluorenones. ChemistrySelect, 5(34), 10673-10691. Impact Factor (2.109)
24. Shantanu, P. A., Sharma, D., Sharma, M., Vaidya, S., Sharma, K., Kalia, K., Shard, A., & Tiwari, V. 2019. Kinesins: Motor Proteins as Novel Target for the Treatment of Chronic Pain. Molecular neurobiology, 56(6), 3854-3864. Impact Factor (5.590)
25. Rawat, K., Shard, A., Jadhav, M., Gandhi, M., Anand, P., Purohit, R., …& Sinha, A. K. (2019). Styryl-cinnamate hybrid inhibits glioma by alleviating translation, bioenergetics and other key cellular responses leading to apoptosis. Experimental cell research, 375(1), 11-21. Impact Factor (3.905)
26. Patel, S., Patle, R., Parameswaran, P., Jain, A., & Shard, A. (2019). Design, computational studies, synthesis and biological evaluation of thiazole-based molecules as anticancer agents. European Journal of Pharmaceutical Sciences, 134, 20-30. Impact Factor (4.384)
27. Rihan, M., Nalla, L. V., Dharavath, A., Shard, A., Kalia, K., & Khairnar, A. (2019). Pyruvate kinase M2: a metabolic bug in re-wiring the tumor microenvironment. Cancer Microenvironment, 12(2), 149-167.
28. Jarial, R., Thakur, S., Sakinah, M., Zularisam, A. W., Shard, A., Kanwar, S. S., & Singh, L. 2018. Potent anticancer, antioxidant and antibacterial activities of isolated flavonoids from Asplenium nidus. Journal of King Saud University-Science, 30(2), 185-192. Impact Factor (4.011)
29. Jarial, R., Shard, A., Thakur, S., Sakinah, M., Zularisam, A. W., Rezania, S., …& Singh, L. 2018. Characterization of flavonoids from fern Cheilanthestenuifolia and evaluation of antioxidant, antimicrobial and anticancer activities. Journal of King Saud University-Science, 30(4), 425-432. Impact Factor (4.011)
30. Biswas, N. M., Shard, A., Patel, S., &Sengupta, P. 2018. Drug development and bioanalytical method validation for a novel anticancer molecule, 4-(dimethylamino)-2-(p-tolylamino) thiazole-5-carbonitrile. Drug development research, 79(8), 391-399. Impact Factor (4.360)
31. Nemani, K. S., Shard, A., & Sengupta, P. 2018. Establishment of a quantitative bioanalytical method for an acetylcholinesterase inhibitor Ethyl 3-(2-(4-fluorophenyl) amino)-4-phenylthiazol-5-yl)-3-oxopropanoate including its physicochemical characterization and in vitro metabolite profiling using Liquid Chromatography-Mass Spectrometry. Journal of Chromatography B, 1096, 214-222. Impact Factor (3.205)
32. Shard, A., Kumar, R., Equbal, D., & Sinha, A. K. 2018. Pot‐Economical Synthesis of Hydroxylated Arylethenyl-arylethynyl-arenes through Sequential Decarboxylative Perkin–Sonogashira Reactions. Asian Journal of Organic Chemistry, 7(1), 189-196. Impact Factor (3.319)
33. Shard, A., Rawat, K., Sinha, A. K., Padwad, Y., & Kumar, D. 2016. Divergent synthesis of styryl–cinnamate hybrid analogues inspired by the natural product salvianolic acid F as a premise to investigate their anticancer activity and its metabolomic profiling. European Journal of Organic Chemistry, 2016(36), 5941-5949. Impact Factor (3.021)
34. Sharma, N., Mohanakrishnan, D., Shard, A., Sharma, A., Sinha, A. K., &Sahal, D. 2016. Hydroxylated di-and tri-styrylbenzenes, a new class of antiplasmodial agents: discovery and mechanism of action. RSC advances, 6(55), 49348-49357. Impact Factor (3.361)
35. Kumar, R., Shard, A., Andhare, N. H., & Sinha, A. K. 2015. Thiol–Ene “Click” Reaction Triggered by Neutral Ionic Liquid: The “Ambiphilic” Character of [hmim] Br in the Regioselective Nucleophilic Hydrothiolation. AngewandteChemie, 127(3), 842-846. Impact Factor (15.336)
36. Shard, A., Kumar, R., Sharma, N., & Sinha, A. K. 2014. Amino acid and water-driven tunable green protocol to access S–S/C–S bonds via aerobic oxidative coupling and hydrothiolation. Rsc Advances, 4(63), 33399-33407. Impact Factor (3.361)
37. Kumar, R., Andhare, N. H., Shard, A., & Sinha, A. K. 2014. Multicomponent diversity-oriented synthesis of symmetrical and unsymmetrical 1, 4-dihydropyridines in recyclable glycine nitrate (GlyNO 3) ionic liquid: a mechanistic insight using Q-TOF, ESI-MS/MS. RSC Advances, 4(37), 19111-19121. Impact Factor (3.361)
38. Kumar, R., Andhare, N. H., Shard, A., & Sinha, A. K. 2013. Water Compatible Multicomponent Cascade Suzuki/Heck–Aldol, Suzuki–Aldol–Suzuki, and Aldol–Suzuki–Aldol Reactions: An Ecofriendly Paradigm for Multiple Carbon-Carbon Bond Formation in One Pot. Chemistry–A European Journal, 19(44), 14798-14803. Impact Factor (5.236)
39. Sharma, N., Mohanakrishnan, D., Shard, A., Sharma, A., Sinha, A. K., &Sahal, D. 2012. Stilbene–chalcone hybrids: design, synthesis, and evaluation as a new class of antimalarial scaffolds that trigger cell death through stage specific apoptosis. Journal of medicinal chemistry, 55(1), 297-311. Impact Factor (7.446)
40. Kumar, R., Sharma, P., Shard, A., Tewary, D. K., Nadda, G., & Sinha, A. K. 2012. Chalcones as promising pesticidal agents against diamondback moth (Plutella xylostella): microwave-assisted synthesis and structure–activity relationship. Medicinal Chemistry Research, 21(6), 922-931. Impact Factor (1.965)
41. Shard, A., Sharma, N., Bharti, R., Dadhwal, S., Kumar, R., & Sinha, A. K. 2012. Tandem Heck/Decarboxylation/Heck Strategy: Protecting‐Group‐Free Synthesis of Symmetric and Unsymmetric Hydroxylated Stilbenoids. AngewandteChemie, 124(49), 12416-12419. Impact Factor (15.336)
42. Kumar, R., Shard, A., Bharti, R., Thopate, Y., & Sinha, A. K. 2012. Palladium‐Catalyzed Dehydrative Heck Olefination of Secondary Aryl Alcohols in Ionic Liquids: Towards a Waste‐Free Strategy for Tandem Synthesis of Stilbenoids. AngewandteChemie International Edition, 51(11), 2636-2639. Impact Factor (15.336)
43. Kumar, R., Sharma, N., Sharma, U. K., Shard, A., & Sinha, A. K. 2012. First Metal‐and Base‐Free Selective Oxidative Coupling of Thiols in Neat Ionic Liquids: NMR Probed “Ambiphilic” Character of Neutral [hmim] Br towards Atom‐Efficient Synthesis of Disulfides. Advanced Synthesis & Catalysis, 354(11‐12), 2107-2112. Impact Factor (5.837)
44. Sharma, A., Sharma, N., Shard, A., Kumar, R., Mohanakrishnan, D., Sinha, A. K., &Sahal, D. 2011. Tandem allylic oxidation–condensation/esterification catalyzed by silica gel: an expeditious approach towards antimalarial diaryldienones and enones from natural methoxylatedphenylpropenes. Organic &biomolecular chemistry, 9(14), 5211-5219. Impact Factor (3.876)
45. Sharma, N., Sharma, A., Shard, A., Kumar, R., & Sinha, A. K. 2011. Pd‐Catalyzed Orthogonal Knoevenagel/Perkin Condensation–Decarboxylation–Heck/Suzuki Sequences: Tandem Transformations of Benzaldehydes into Hydroxy‐Functionalized Antidiabetic Stilbene–Cinnamoyl Hybrids and Asymmetric Distyrylbenzenes. Chemistry–A European Journal, 17(37), 10350-10356. Impact Factor (5.236)
46. Sharma, A., Sharma, N., Kumar, R., Shard, A.,& Sinha, A. K. 2010. Direct olefination of benzaldehydes into hydroxy functionalized oligo (p-phenylenevinylene) s via Pd-catalyzed heterodominoKnoevenagel-decarboxylation-Heck sequence and its application for fluoride sensing π-conjugated units. Chemical Communications, 46(19), 3283-3285. Impact Factor (6.222)
47. Sharma, N., Sharma, A., Kumar, R., Shard, A., & Sinha, A. K. 2010. One‐Pot Two‐Step Oxidative Cleavage of 1, 2‐Arylalkenes to Aryl Ketones Instead of Arylaldehydes in an Aqueous Medium: A Complementary Approach to Ozonolysis. European Journal of Organic Chemistry, 6025-6032 Impact Factor (3.021)
48. Sinha, A. K., Sharma, N., Shard, A., Sharma, A., Kumar, R., & Sharma, U. K. 2009. Green methodologies in synthesis and natural product chemistry of phenolic compounds. Indian journal of Chemistry, 48B(12), 1771-1779. Impact Factor (0.592)

Book Chapter: Das, Rudradip, Hansal Kumar, Asmita Choithramani, GouravBothra, and Shard, A. “Polymeric Nanoparticles to Entrap Natural Drugs for Cancer Therapy.” Polymeric nanoparticles for the treatment of solid tumors (2022): 167-211.DOI: 10.1007/978-3-031-14848-4_6.

Research Scholars

Student Details

Moumita Ghosh Chowdhury

Ms. Moumita Ghosh Chowdhury received her B Pharm degree from West Bengal University of Technology, Kolkata, India, in 2017. She received her MS (Pharm) degree in Medicinal Chemistry from NIPER Mohali in 2020. Currently, she is pursuing a PhD in medicinal chemistry from National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad, India, under the guidance of Dr. Amit Shard. Her current research interest focuses on designing, synthesizing and evaluation N-heterocyclic compounds as potent PKM2 modulators.

Rudradip Das

Mr. Rudradip Das received his B. Pharm degree in Pharmaceutical Technology from West- Bengal University of Technology, Kolkata, India in 2017, he received his M.S. (Pharm.) degree in Medicinal Chemistry from NIPER-Mohali in 2019. Currently, he is pursuing a Ph.D. in Medicinal Chemistry from the National Institute of Pharmaceutical Education and Research (NIPER) Ahmedabad, India under the guidance of Dr. Amit Shard. His current research interest is the design, synthesis, and evaluation of small organic compounds as potential agents against PKM2.

Saumya Kapoor

Ms. Saumya Kapoor received her B. Pharm degree from UIPS Punjab University, Chandigarh in 2019. She received her M.S. (Pharm.) degree in Medicinal Chemistry from NIPER-Mohali in 2021. Currently, she is pursuing a Ph.D. in Medicinal Chemistry from the National Institute of Pharmaceutical Education and Research (NIPER) Ahmedabad, India. Her area of research is Design, Synthesis and Biological Evaluation of Imidazopyridazines as novel PKM2 Modulators.

Deep Rohan Chatterjee

Deep Rohan Chatterjee pursued his graduation from Gurunanak Institute of Pharmaceutical Science & Technology (GNIPST) under Maulana Abul Kalam Azad University of Technology (formerly the West Bengal University of Technology), and received his B. Pharm. degree from Maulana Abul Kalam Azad University of Technology (formerly the West Bengal University of Technology), West Bengal, India, in 2018. Subsequently, he received his MS (Pharm.) degree in Medicinal Chemistry under the guidance of Dr. Dinesh Kumar from the National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad, India, in 2020. Currently, he is pursuing his doctoral degree in Medicinal Chemistry from the National Institute of Pharmaceutical Education and Research (NIPER), Ahmedabad, India, under the guidance of Dr. Amit Shard. His current research interest focuses on designing, synthesizing, and evaluating novel PKM2 modulators as well as PROTACs as anticancer agents.

Shailendra Sharma

Mr. Shailendra Sharma received his B.Sc. in biology from Kanpur university Uttar Pradesh India in 2015, he received his M. Sc. in chemistry from Kanpur university Uttar Pradesh, India in 2017. Currently, He is pursuing a Ph.D. in medicinal chemistry from the National institute of pharmaceutical education and research (NIPER) Ahmedabad, India under the guidance of Dr. Amit shard. He is working on API Synthesis using sustainable methods.

Vaishnavi Kalmegh

Ms. Vaishnavi Kalmegh received her B.Pharm Degree from Sant Gadge Baba Amravati University, in 2020. She received her M.S.(Pharm) in Medicinal Chemistry under the guidance of Dr. Murali Mohan Guru from NIPER – Kolkata in 2022. Currently, she is pursuing Ph.D in Medicinal Chemistry, under the mentorship of Dr. Amit Shard from National Institute of Pharmaceutical Education and Research (NIPER) Ahmedabad. Her ongoing research topic focuses on the design, synthesis, and biological evaluation of Hetero-aromatic derivatives as PKM2 modulators.

Madhav Shivdarshan Jadhav

Mr. Madhav Shivdarshan Jadhav, has completed his B. Pharmacy at Dayanand College of Pharmacy, Latur (Maharashtra), India in 2020. He Later Earned his M. Pharmacy from Bharti Vidyapeeth Deemed to be University’s Poona College of Pharmacy, Pune (Maharashtra), India in 2022. Currently he is working as Junior Research Fellow at National Institute of Pharmaceutical education and Research (NIPER) Ahmedabad, on a GSBTM sponsored project on the Design, Synthesis & evaluation of novel Quinazolinone derivatives as Pyruvate Kinase M2 modulators.

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