RESEARCH INTERESTS

Synthetic Organic Chemistry, Bioorganic Chemistry, Chemical Biology

ABOUT/BIOGRAPHY

Dr. Pitsinos obtained his B.Sc. in chemistry from the Aristotle University of Thessaloniki (Greece) in 1988. Upon graduation he worked for one year as research assistant in the group of Prof. M. Papadopoulos at the University of Crete and then he joined the group of Prof. K. C. Nicolaou at the University of California, San Diego / The Scripps Research Institute (San Diego, USA) to pursue his PhD on the total synthesis of the enediyne antibiotic Calicheamicin and the synthesis / biological evaluation of related analogues. He was also involved in the synthesis of water-soluble derivatives of the anticancer agent Paclitaxel (Taxol™). After a two-year service in the Greek Army, he was actively involved, as a post-doctoral fellow in the group of Prof. E. A. Couladouros, in setting up a new activity on “Synthetic Organic & Bioorganic Chemistry” in the Institute of Physical Chemistry, NCSR “Demokritos” (Greece). In 1997, he joined as Marie Curie Fellow the group of Prof. J.-M. Lehn at the University of Strasbourg (France) where he pursued the preparation of supramolecular assemblies through hydrogen bonding. In 1999, he returned as Researcher C level to NCSR “Demokritos”. He has pursued the synthesis and study of several natural products (Bastadins, Scyphostatin, Oxazines, Laurenditerpenol) and has established a network of national and international collaborations (e.g., Prof. E. A. Couladouros, Prof. S. Haroutounian, Agricultural University of Athens; Prof. E. Fattorusso, Universita degli Studi di Napoli ‘Federico II’; Prof. A. Giannis, University of Leipzig; Prof. E.-I. Negishi, Purdue University; Prof. K. C. Nicolaou, W. M. Rice University).

He is currently Research Director (Researcher A level), responsible for the “Natural Products Synthesis & Bioorganic Chemistry” group at the Institute of Nanoscience & Nanotechnology, NCSR “Demokritos”.

Representative Publications

  1. “Total synthesis of (+)-Scyphostatin featuring an enantioselective and highly efficient route to the side-chain via Zr-catalyzed asymmetric carboalumination of alkenes (ZACA)”
    E. N. Pitsinos, N. Athinaios, Z. Xu, G. Wang, E.-I. Negishi,
    Chemical Communications 2010, 46, 2200–2202.
  2. “Diaryl ether formation in the synthesis of natural products”
    E. N. Pitsinos, V. P. Vidali, E. A. Couladouros,
    European Journal of Organic Chemistry 2011, 1207–1222.
  3. “Enantioselective total synthesis of (–)-Laurenditerpenol”
    E. N. Pitsinos, N. Athinaios, V. P. Vidali,
    Organic Letters 2012, 14, 4666–4669.
  4. “A fast entry to furanoditerpenoid-based Hedgehog signaling inhibitors: Identifying essential structural features”
    M. Chatzopoulou, A. Antoniou, E. N. Pitsinos, M. Bantzi, S. D. Koulocheri, S. A. Haroutounian, A. G. Giannis,
    Organic Letters 2014, 16, 3344−3347.
  5. “Identification of Gli-mediated transcription inhibitors through synthesis and evaluation of Taepeenin D analogues”
    A. Antoniou, M. Chatzopoulou, M. Bantzi, C. M. Athanassopoulos, A. G. Giannis, E. N. Pitsinos,
    MedChemComm 2016, 7, 2328−2331.
  6. “Total synthesis and full structural assignment of Namenamicin”
    K. C. Nicolaou, R. Li, Z. Lu, E. N. Pitsinos, L. B. Alemany,
    Journal of the American Chemical Society 2018, 140, 8091−8095.

https://orcid.org/0000-0003-0626-0578

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PUBLICATIONS

Nicolaou, K. C., Rigol, Stephan, Pitsinos, Emmanuel N., Das, Dipendu, Lu, Yong, Rout, Subhrajit, Schammel, Alexander W. and Holte, Dane, Lin, Baiwei, Gu, Christine, Sarvaiya, Hetal and Trinidad, Jose, Barbour, Nicole, Valdiosera, Amanda M. and Sandoval, Joseph, Lee, Christina, Aujay, Monette, Fernando, Hanan, Dhar, Anukriti, Karsunky, Holger, Taylor, Nicole and Pysz, Marybeth and Gavrilyuk, Julia, Uncialamycin-based antibody-drug conjugates: Unique enediyne ADCs exhibiting bystander killing effect PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, Volume 118, 2021 [doi]

Nicolaou, K. C., Li, Ruofan, Chen, Qifeng, Lu, Zhaoyong and Pitsinos, Emmanuel N., Schammel, Alexander, Lin, Baiwei, Gu, Christine, Sarvaiya, Hetal, Tchelepi, Robert, Valdiosera, Amanda, Clubb, Justin, Barbour, Nicole, Sisodiya, Vikram and Sandoval, Joseph, Lee, Christina, Aujay, Monette and Gavrilyuk, Julia, Synthesis and Biological Evaluation of Shishijimicin A-Type Linker-Drugs and Antibody-Drug Conjugates JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Volume 142, Pages: 12890-12899, 2020 [doi]

Pitsinos, Emmanuel N., Mavridis, Ioannis and Tzouma, Eirini and Vidali, Veroniki P., Enantioselective Synthesis of Cassane-Type Furanoditerpenoids: Total Synthesis of Sucutiniranes C and D EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Volume 2020, Pages: 4730-4742, 2020 [doi]

Nicolaou, K. C., Das, Dipendu, Lu, Yong, Rout, Subhrajit and Pitsinos, Emmanuel N., Lyssikatos, Joseph, Schammel, Alexander and Sandoval, Joseph, Hammond, Mikhail, Aujay, Monette and Gavrilyuk, Julia, Total Synthesis and Biological Evaluation of Tiancimycins A and B, Yangpumicin A, and Related Anthraquinone-Fused Enediyne Antitumor Antibiotics JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Volume 142, Pages: 2549-2561, 2020 [doi]

Zhang, Hao, Li, Ruofan, Ba, Sai, Lu, Zhaoyong, Pitsinos, Emmanuel N., Li, Tianhu and Nicolaou, K. C., DNA Binding and Cleavage Modes of Shishijimicin A JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Volume 141, Pages: 7842-7852, 2019 [doi]

Nicolaou, K. C., Li, Ruofan, Lu, Zhaoyong, Pitsinos, Emmanuel N., Alemany, Lawrence B., Aujay, Monette, Lee, Christina and Sandoval, Joseph and Gavrilyuk, Julia, Streamlined Total Synthesis of Shishijimicin A and Its Application to the Design, Synthesis, and Biological Evaluation of Analogues thereof and Practical Syntheses of PhthNSSMe and Related Sulfenylating Reagents JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Volume 140, Pages: 12120-12136, 2018 [doi]

Nicolaou, K. C., Li, Ruofan, Lu, Zhaoyong, Pitsinos, Emmanuel N. and Alemany, Lawrence B., Total Synthesis and Full Structural Assignment of Namenamicin JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Volume 140, Pages: 8091-8095, 2018 [doi]

Antoniou, A., Chatzopoulou, M., Bantzi, M., Athanassopoulos, C. M., Giannis, A. and Pitsinos, E. N., Identification of Gli-mediated transcription inhibitors through synthesis and evaluation of taepeenin D analogues MEDCHEMCOMM, Volume 7, Pages: 2328-2331, 2016 [doi]

Tzouma, Eirini, Mavridis, Ioannis and Vidali, Veroniki P. and Pitsinos, Emmanuel N., Diels-Alder reaction between 1,3,3-trisubstituted-2-vinylcyclohexenes and quinones under exceptionally mild conditions: a concise entry to the cassane-type furanoditerpenoid skeleton TETRAHEDRON LETTERS, Volume 57, Pages: 3643-3647, 2016 [doi]

Nicolaou, K. C., Wang, Yanping, Lu, Min, Mandal, Debashis and Pattanayak, Manas R., Yu, Ruocheng, Shah, Akshay A., Chen, Jason S., Zhang, Hongjun, Crawford, James J., Pasunoori, Laxman, Poudel, Yam B., Chowdari, Naidu S., Pan, Chin, Nazeer, Ayesha, Gangwar, Sanjeev, Vite, Gregory and Pitsinos, Emmanuel N., Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Volume 138, Pages: 8235-8246, 2016 [doi]

Chatzopoulou, Maria, Antoniou, Antonia, Pitsinos, Emmanuel N. and Bantzi, Marina, Koulocheri, Sofia D. and Haroutounian, Serkos A. and Giannis, Athanassios, A Fast Entry to Furanoditerpenoid-Based Hedgehog Signaling Inhibitors: Identifying Essential Structural Features ORGANIC LETTERS, Volume 16, Pages: 3344-3347, 2014 [doi]

Michaelakis, Antonios, Vidali, Veroniki P., Papachristos, Dimitrios P., Pitsinos, Emmanuel N., Koliopoulos, George and Couladouros, Elias A., Polissiou, Moschos G. and Kimbaris, Athanasios C., Bioefficacy of acyclic monoterpenes and their saturated derivatives against the West Nile vector Culex pipiens CHEMOSPHERE, Volume 96, Pages: 74-80, 2014 [doi]

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