Bioheterocycles 2015

PL04 - Non Noble Metal Catalysis for Making Precious Molecules

Prof. Matthias BELLER

UNIVERSITY OF ROSTOCK, Rostock, Germany
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Prof. Matthias BELLER

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http://www.catalysis.de/Beller-Matthias.239.0.html

Matthias Beller, born 1962 in Gudensberg, studied chemistry at the University of Göttingen, Germany, where he completed his PhD thesis in 1989 in the group of L.-F. Tietze. As recipient of a Liebig scholarship, he then spent a one-year with K. B. Sharpless at MIT, USA. From 1991 to 1995, Beller worked in industry. Then, he moved to the Technical University of München as Professor for Inorganic Chemistry. In 1998, he relocated to Rostock to head the Institute for Organic Catalysis, which became in 2006 the Leibniz-Institute for Catalysis. The work of his group has been published in >650 original publications, reviews and >90 patent applications have been filed in the last decade. He has received several awards including the Otto-Roelen Medal and the Leibniz-Price of the DFG. In 2006, he was also awarded “Entrepreneur of the Year” of Rostock and he received the German Federal Cross of Merit. Since then, he received the first “European price for Sustainable Chemistry”, the “Paul-Rylander Award” of the Organic Reaction Catalysis Society of the USA, the Gay-Lussac-Alexander-von-Humboldt-Prize of the French Academy of Sciences and the Emil Fischer Medal of the German Chemical Society. Matthias Beller is head of the German Chemical Society working group “Sustainable Chemistry” and a member of the German National Academia of Science “Leopoldina”. He is married to Dr. Anja Fischer-Beller and they have two sons.

PL08 - Heterocycles Derived from Natural Products in Management of Multidrug Resistance

Prof. Ahcene BOUMENDJEL

UNIVERSITÉ JOSEPH FOURIER, La Tronche, France
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Prof. Ahcene BOUMENDJEL

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Ahcène BOUMENDJEL is a professor of medicinal chemistry at the Faculty of Pharmacy of Grenoble, France and he is the head of the medicinal chemistry laboratory. His research field deals with the chemistry of natural products with a special focus on the design, synthesis and development of drug candidates. Professor BOUMENDJEL obtained his PhD of organic chemistry in 1991 from the University of Reims (France). After a postdoctoral fellow at the National Institutes of Health (Bethesda, USA) he spent two years working for a Biotech company. In 1996, he was appointed as a professor assistant in pharmacognosy at the Faculty of Pharmacy of Grenoble and in 2008, he became a full Professor of medicinal chemistry.

PL05 - Metal Catalysis for Heteroarene Synthesis

Prof. Michael GREANEY

THE UNIVERSITY OF MANCHESTER, Manchester, United Kingdom
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Prof. Michael GREANEY

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Michael Greaney took his undergraduate degree at Oxford, completing his part II research project in the group of Sir Jack Baldwin in 1996. He then moved to London to carry out PhD work with William Motherwell at UCL, completing his thesis in the area of new fluorinating agents in 1999. He then left the UK on a GlaxoWellcome scholarship to take up a postdoctoral position with Jeffrey Winkler at the University of Pennsylvania, where he worked on the total synthesis of the tumour-promoting diterpene ingenol. He returned to the UK in early 2002, to a lectureship position at the University of Edinburgh. He was awarded an EPSRC Leadership Fellowship in 2008, and in 2011 moved to the University of Manchester to a personal chair in organic chemistry.

PL06 - The Discovery and Development of the HIV Intergrase Inhibitors Dolutegravir and Cabotegravir

Dr Brian JOHNS

GLAXOSMITHKLINE, NC, United States
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Dr Brian JOHNS

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Dr Johns received a Ph.D. from Wayne State University in Detroit in 1997 under the direction of Professor Carl R. Johnson working on chemoenzymatic methodology to make bioactive aza-C-disaccharides. He continued his training as an NIH postdoctoral fellow at the University of Virginia in Charlottesville under the direction of Professor James A. Marshall where he completed a total synthesis of the polyketide natural product discodermolide using allenyl metal methodology to establish key stereotriad motifs. Dr. Johns then joined GlaxoWellcome (now GSK) in Research Triangle Park, North Carolina in 1999 as part of the virology chemistry group where he continues today. Dr Johns is an author or co-author of 45 peer reviewed journal articles and an inventor on 49 patents and patent applications. He currently holds the title Director of HIV Medicinal Chemistry and DMPK within the infectious diseases therapy area unit at GlaxoSmithKline.

PL07 - Bronsted Acid and Metal-catalyzed Reactions in the Synthesis of Heterocycles

Prof. Esther LETE

UNIVERSIDAD DEL PAÍS VASCO, Bilbao, Spain
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Prof. Esther LETE

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Prof. Dr. Esther Lete is Professor of Organic Chemistry at the Department of Organic Chemistry, Faculty of Science and Technology, University of the Basque Country, UPV/EHU, Bilbao (Spain). She obtained a first class honours degree in Chemistry at the University of Bilbao in 1978. She received a PhD degree at the University of the Basque Country in 1982 with a thesis on synthesis of 3-arylisoquinolines (supervisor. E. Domínguez). In 1982 she carried out a postdoctoral research with P. J. Garrat at University College London, studying the chemistry and synthetic applications of carbanions. Then, she took up a lectureship in organic chemistry at the University of the Basque Country and was promoted to Full Professor in 1997. Her current research interests include organometallic chemistry and asymmetric synthesis. She is now involved in the development of stereo- and enantioselective strategies of C-C bond forming reactions for the synthesis of heterocyclic systems. Especially she is concerned with synthetic methodologies based on carbolithiation, alpha-amidoalkylation, Heck and C-H functionalization reactions. For additional information: www.ehu.es/oms

PL01 - Photoreactive Heterocycles and Natural Product Derivatives

Prof. Dr Thomas LINDEL

TECHNICAL UNIVERSITY OF BRAUNSCHWEIG, Braunschweig, Germany
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Prof. Dr Thomas LINDEL

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Thomas Lindel (born 1966) studied chemistry at the University of Münster, Germany, where he received his doctorate in 1992 with Burchard Franck. After postdoctoral studies with William Fenical at the Scripps Institution of Oceanography (La Jolla, USA) he moved to the laboratories of Richard Neidlein at the Institute of Pharmaceutical Chemistry, University of Heidelberg. In 2000, Thomas Lindel obtained his habilitation for organic chemistry. In 2001, he became Associate Professor at the Department of Chemistry and Biochemistry, LMU Munich. Since 2007, Thomas Lindel has been Full Professor of Organic Chemistry at the Faculty of Life Sciences at TU Braunschweig, Germany. His research covers the total synthesis of marine alkaloids, terpenoids, and peptides, and the chemistry of photoaffinity labeling.

PL02 - Targeting DNA Methylation: a Medicinal Chemistry Approach

Prof. Antonello MAI

UNIVERSITY OF ROME "LA SAPIENZA", Rome, Italy
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Prof. Antonello MAI

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Antonello Mai was born in Rome, Italy, in November 14th 1962. He took the Degree in Pharmacy at the Sapienza University of Rome (110/110 cum laude). From 1989 to 1992, he made the PhD course in Medicinal Chemistry and Pharmaceutical Sciences, Sapienza University of Rome, and in 1992 he took his PhD in Medicinal Chemistry and Pharmaceutical Sciences. From 1998 to 2010, Antonello Mai worked as a Associate Professor in the Faculty of Pharmacy (Department of Pharmaceuticals Studies) at the University of Rome “La Sapienza”. In 2011 he was been appointed as Full Professor in Medicinal Chemistry at Sapienza University of Rome. Antonello Mai is professor of the following courses at the Faculty of Pharmacy and Medicine of Sapienza University of Rome involving Medicinal Chemistry and Toxicology Analysis, Pharmaceutical Biotechnology. He has great expertise in 1) organic synthesis; 2) synthesis of new potential bio-active compounds, particularly in the field of epigenetics (inhibitors of DNMTs, HDACs [unselective and class-selective], HATs, sirtuins, PRMTs, HKMTs, and HDs), anticancer agents, antiviral agents (anti-human picornavirus compounds (disoxaril analogues), and anti-HIV-1 compounds belonging to the non-nucleoside reverse transcriptase inhibitor classes (DABOs, S-DABOs, DATNOs, F2-S-DABOs, Amino-DABOs), antibacterial (oxacine analogues), antimycobacterial (oxacine and U-100480 analogues) and antifungal (trichostatin A, pyrrolnitrin, and bifonazole analogues) agents, and CNS agents (pyrrolobenzodiazepines active as analgesic, antidepressant and nootropic compounds); 3) development of new methodology for the synthesis of heterocycles; 4) analysis and purification of organic mixtures; 5) study and characterization of organic molecules.

PL03 - The Importance of Heterocycles in Agrochemistry: Fungicides as a Case Study

Dr Harald WALTER

SYNGENTA CROP PROTECTION AG BASEL, Basel, Switzerland
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Dr Harald WALTER

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After having received a Ph.D. in organic chemistry from the University of Tübingen (Germany) in 1985, Harald joined the dyestuff division of former Ciba-Geigy AG. In 1990 he joined the agro divison of Ciba-Geigy and worked there as a team resp. project leader in the fungicide area. After several mergers (Ciba-Geigy + Maag AG + Sandoz AG + Zeneca (agro part)), Syngenta Crop Protection AG was formed in the year 2000. Within Syngenta Harald worked as a senior project leader and was appointed to Syngenta Fellow (member of the scientific career ladder of Syngenta) in 2003. He was appointed to leader of the portfolio strategy team fungicides in 2008 and is currently research portfolio manager for fungicides and new technologies.
Publications:
More than 140 journal papers and patent applications (major topics: heterocyclic chemistry, new agrochemical fungicides). Two chapters in books, topics: complex I and complex II inhibitors)

IL07 - Silicon-Containing Tetrahydrocyclopenta[C]Acridine Derivatives as CDKs Inhibitors: Design, Organometallic Synthesis, Metabolic Stability And Optimization

Prof. Philippe BELMONT

UNIVERSITY PARIS DESCARTES, Paris, France
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Prof. Philippe BELMONT

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Philippe Belmont was born in Paris in 1970. He grew up in the French Caribbean where he started a BS degree in Biology and Biochemistry. In 1990 he moved to the University Joseph Fourier (Grenoble, France), where in 1996 he obtained a PhD in Bioorganic Chemistry (Advisor: Dr M. Demeunynck/Pr J Lhomme). Then, he moved successively as a post-doctoral fellow at Case Western Reserve University (Professor A. J. Pearson, Cleveland, USA) and to the Collège de France (Pr J.-M. Lehn/Dr J.-P. Vigneron, Paris, France). In 2000 he joined the group of Pr M. A. Ciufolini as a CNRS researcher (ICBMS Intitute, UMR CNRS 5246, Lyon, France). He obtained in 2004 the habilitation diploma and started then an autonomous career. In 2009, Philippe Belmont was awarded the CNRS bronze medal and then joined the Institut Curie (UMR CNRS 176, Paris, France) with a joint CNRS/INCa ATIP fellowship to lead an independent research group. In 2011 he succeeded in becoming a CNRS senior researcher (DR2 CNRS), but chose the same year an appointment as a full Professor of organic chemistry at the Université Paris Descartes, School of Pharmacy (UMR CNRS 8638). His field of interest and expertise are in organometallic chemistry (Au, Ag, Co, Rh) devoted to the original access to various heterocyclic structures in view of studying their biological properties, in particular against tumors (e.g. kinases inhibition)

IL01 - Synthetic Explorations in Small-ring Azaheterocyclic Chemistry and Development of Novel Bioactive Heterocycles

Prof. Matthias D'HOOGHE

GHENT UNIVERSITY, Ghent, Belgium
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Prof. Matthias D'HOOGHE

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Matthias D’hooghe was born in Kortrijk, Belgium, in 1978. He received his Master’s diploma in 2001 (Master of Science in Bioscience Engineering: Chemistry) and his PhD degree in 2006 (Doctor in Applied Biological Sciences: Chemistry), both from Ghent University, Belgium, with Prof. N. De Kimpe as promoter. In 2007, he became Assistant Professor at the Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, and in 2009 he performed a short postdoctoral stay with Prof. D. Vogt at Eindhoven University of Technology (The Netherlands) in the field of homogeneous catalysis. In October 2010, he was promoted to Associate Professor (Research Professor) at the Department of Sustainable Organic Chemistry and Technology (Ghent University). His main research interests include the chemistry of small-ring azaheterocycles, with a special focus on aziridines, azetidines and b-lactams, and the synthesis of different classes of bioactive heterocyclic compounds. Prof. D’hooghe has been elected as a laureate of the DSM Science & Technology Awards 2007, finalist of the European Young Chemist Award 2012 and recipient of the Thieme Chemistry Journal Award 2013.

IL09 - Overcoming Resistance with beta-Lactams

Dr Eric DESARBRE

BASILEA PHARMACEUTICA, Basel, Switzerland
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Dr Eric DESARBRE

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Dr Eric Desarbre obtained his PhD in 1995 from University of Orléans (France) under the supervision of Pr. Jean-Yves Merour for the preparation of pyrrolo[2,3-b]pyridine derivatives (7-azaindoles). He then joined Pr. Jan Bergman’s department at the Karolinska Institute (Stockholm, Sweden) for a post-doctoral position where he prepared indolo[2,3-c]carbazole moieties. After 5 years at Pharmacia Corporation (Stockholm, Sweden) he joined the research department of Basilea Pharmaceutica (Basel, Switzerland) in 2001 where he is involved in antimicrobial projects. As deputy project leader and responsible of the chemist team for Gram-negative antibacterial projects since 2004, he is now working with -lactam substances which recently led to the discovery of monobactam antibiotic BAL30072.

IL08 - At the Crossroads of Chemistry and Biology: Inhibiting Protein Kinase CK2 by Heterocyclic Small Molecules

Prof. Marc LE BORGNE

UNIVERSITÉ CLAUDE BERNARD LYON 1, Lyon, France
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Prof. Marc LE BORGNE

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Current title and position: Director of the Research Team EA 4446 “Biomolecules Cancer Chemoresistances” (B2C), Université Claude Bernard Lyon 1 and Professor in Medicinal Chemistry, Faculty of Pharmacy-Institut des Sciences Pharmaceutiques et Biologiques (ISPB), Lyon (France).
Research field: Design, synthesis and structural optimization of functionalized small molecules as anticancer agents (CK2, Dyrks, Aurora), efflux pump inhibitors (P-gp, BCRP) and anti-infective agents (CYP51). Some scaffolds developed: indole, naphthyridine, indeno[1,2-b]indole.
Education and former professional experience: teaching experience in medicinal chemistry (design, synthesis, optimization, SAR analysis, ADMET, therapeutic uses), drug lifecycle and industrial property rights. Junior lecturer at University of Nantes (France, 1999-2008).

IL06 - Utilization of Hypervalent Iodonium Reagents for the Construction and Functionalization of Heterocyclic Molecules

Dr Zoltan NOVAK

EÖTVÖS UNIVERSITY, Budapest, Hungary
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Dr Zoltan NOVAK

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Zoltán Novák studied chemistry at the Eötvös University, Budapest, Hungary, and received his diploma in 1999 and his PhD in 2004 (with Prof. András Kotschy). He then moved to the California Institute of Technology and performed postdoctoral research in the laboratory of Prof. Brian M. Stoltz. From 2006, he continued his postdoctoral research at the Eötvös University. In 2007, he started his independent career at the Institute of Chemistry, Eötvös University Budapest as an Assistant Professor. His research mainly focuses to synthesis and utilization of hypervalent iodine reagents, and the development of transition metal catalyzed transformations, such as cross-coupling and C-H activation for the construction and functionalization of aromatic and heterocyclic systems.

IL04 - New Methods in Thioamide Chemistry

Dr Mike PORTER

UNIVERSITY COLLEGE LONDON, London, United Kingdom
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Dr Mike PORTER

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Dr Mike Porter is currently Senior Lecturer in the Department of Chemistry at University College London. He graduated from the University of Oxford in 1992, and remained at the same institution for his D.Phil., studying the biosynthesis of penicillins under the supervision of Prof. Sir Jack Baldwin. Following postdoctoral research at the University of Texas (Prof. Phil Magnus; hypervalent iodine chemistry) and the University of Liverpool (Prof. Stan Roberts; polypeptide-catalysed epoxidation), he started his independent research career at UCL in 1999. His research focuses on the development of new methodology for the synthesis of biologically active compounds and includes aspects of carbene chemistry, manipulation of thiocarbonyls, and visible light photoredox reactions. Recent collaborations have diversified his research into areas such as the preparation of antibacterial polymers, and the time-resolved photoelectron spectroscopy of organic chromophores.

IL05 - Are Generic Drugs Only a Copy_and_Paste Products?

Prof. Stanislav RADL

ZENTIVA, Prague, Czech Republic
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Prof. Stanislav RADL

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A versatile chemist with research, teaching, writing, and editing skills combined with industrial applied research experience.
Graduated from the University of Chemical Technology in Prague (UCT), his PhD obtained at the Czech Academy of Sciences. He has a long history of leading Organic Synthesis Department at the Research Institute of Pharmacy and Biochemistry in Prague and at Zentiva. His main scientific interests include Heterocyclic Chemistry, especially nitrogen-containing heterocycles, and Medicinal Chemistry. Currently employed by Zentiva –A Sanofi Company as a Scientific Development Expert.
He is also engaged at the UCT where he is teaching several drug development related subjects, especially Medicinal Chemistry.

IL03 - Synthesis of Novel Alpha7-nAchR Ligands: from an Idea to in Rodent Results for Alzheimer [18F] TEP Imaging

Prof. Sylvain ROUTIER

UNIVERSITÉ D'ORLÉANS, Orléans, France
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Prof. Sylvain ROUTIER

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Current title and position: Full professor in organic chemistry. Director of a Research Team of UMR 7311 “Heterocyclic and medicinal chemistry”, Univerity of Orléans, France.

Sylvain Routier is born in 1969 in Montreuil sur mer, a nice small town in the north of France. He started his career with a phD n Lille and discovered novel organometallic salen derivatives able to be used as chemical nucleases (Advisors: JL Bernier, JP Catteau, C. Bailly). After a post-doctoral position in collaboration with UCB pharma (homage to P. Talaga), he joined, as assistant professor, the Gerald Guillaumet Group in Orleans and developed novel methodologies in organic synthesis and series for medicinal chemistry and more precisely worked in (aza)indoles chemistry (supervisor : JY Merour). In 2007, he became full professor and leader of a research team (F. Buron, K. Ple, 10 students).

He has received FUI, ANR, INCa and two labex grants (French excellence programs IRON and Synorg) and he has managed the strand valorization of marine product of the Cancéropôle Grand Ouest (19 teams, translationnel projects in oncology: clinic, chemistry, biology…). He is the lead of integrated academic or industrial medicinal chemistry programs which are oriented in the discovery of heterocyclic drugs for innovative medicine (imaging and therapy) and is member of the administrative council of the French Medicinal Chemistry Society (General Secretary Deputy). He is author of 101 publications and patents (http://www.icoa.fr/fr/node/49).

Research fields:
Methodology : organometallic and heteroaromatic chemistry, pseudopeptidic synthesis.
Novel Technologies for organic chemistry: greener process and flow chemistry.
Chemical engineering for health: hit to lead optimization, drug design (Cancer CNS pathologies, Metabolic disorders and inflammatory disease),
Imaging (structural optimization and preparation of innovative substrate for ¹¹C and ¹⁸F radiolabeling).

IL02 - Synthesis of Biorelevant Heterocycles with N-heterocyclic Carbenes

Prof. Andreas SCHMIDT

TECHNICAL UNIVERSITY CLAUSTHAL, Clausthal-Zellerfeld, Germany
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Prof. Andreas SCHMIDT

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1983 – 1989: Studies of Chemistry at the universities of Wuppertal and Bonn, Germany
1992: PhD (Supervisor Prof. Dr. Dr. Heinrich Wamhoff)
2000: Habilitation at University of Greifswald, Germany
1999 - 2000: Postdoc at Emory University, Atlanta, GA (with Prof. Dr. Albert Padwa)
2000 - date :Associate professor / Professor at Clausthal University of Technology
2011 - date: Dean of studies at the faculty of natural and materials sciences of Clausthal University of Technology

Research

N-Heterocyclic carbenes in synthesis and catalysis
Photoresponsive materials
Heterocyclic synthesis
Chemistry of mesomeric betaines

OC10 - Flavylium-Based Pigments – “Click” Synthesis & Biological Relevance

OC16 - Discovery Of Novel Thieno[3,2-b]Pyrrole 5-Carboxamides as Potent Inhibitors of Chikungunya Virus (CHIKV)

OC01 - Heterocycle-Peptide Hybrids: Synthesis, Conformational Analysis, and Utilization in Medicinal Chemistry

OC06 - An Original Domino Radical Cyclisation/Smiles Rearrangement Combination: Application to the Synthesis of Indolo[2,3-b]Quinoline-Type Derivatives

OC05 - Recent Advances in the Total Synthesis of Phormidolides B and C

OC08 - Synthesis of Long Regioregular Dialkyl-Substituted Alpha-Oligofurans

OC15 - Mixed Cu(II) Cu(I) Complexes with Bioheterocycles as the Platform for Construction of Novel Anticancer Agents

OC13 - Synthesis of Imidazo-Pyrrolo-Pyrazines/Diazepines/Diazocines via Domino Ugi/Micheal Reaction and Silver-Catalyzed Heteroannulation

OC11 - Synthesis of 7-(2-Aminophenyl)- and 7-(4-Aminophenyl)Guanine, DNA Adducts Derived from the Phenylnitrenium Ion

OC04 - Novel Cross-Conjugated Dienones Based on 4-Piperidone Moiety: Synthesis and Antitumor Properties

OC03 - Diverse Synthesis of Natural Product Inspired Fused and Spiro-Heterocyclic Scaffolds via Ring Distortion And Construction Strategy

OC02 - Exploiting the Zincke Reaction to Produce Sophisticated Heptamethine Dyes

OC07 - Palladium-Catalyzed Cross-Coupling Reactions in the Asymmetric Synthesis of Pyrrolo[1,2-b]Isoquinolines

OC12 - Heterocyclic Coumarine Analogs as Zinc Metalloprotease Inhibitors