Streamlined Total Synthesis of Trioxacarcins and Its Application to the Design, Synthesis, and Biological Evaluation of Analogues Thereof. Discovery of Simpler Designed and Potent Trioxacarcin Analogues

2017 ◽  
Vol 139 (43) ◽  
pp. 15467-15478 ◽  
Author(s):  
K. C. Nicolaou ◽  
Pengxi Chen ◽  
Shugao Zhu ◽  
Quan Cai ◽  
Rohan D. Erande ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

scholarly journals Total Synthesis Endeavors and Their Contributions to Science and Society:A Personal Account

CCS Chemistry ◽  
2019 ◽  
pp. 3-37 ◽  
Author(s):  
K. C. Nicolaou ◽  
Stephan Rigol ◽  
Ruocheng Yu
Keyword(s):  
Total Synthesis ◽  
Organic Synthesis ◽  
Materials Science ◽  
Biological Evaluation ◽  
Synthetic Methods ◽  
Design Synthesis ◽  
Current State ◽  
Target Molecules ◽  
The 19Th Century ◽  
Synthesis And Biological Evaluation

The advent of organic synthesis in the 19th century, serendipitous as it was, set in motion a revolution in science that continues to evolve into increasing levels of sophistication and to expand into new domains of science and technology for the benefits of science and society. Its evolution was always driven by the challenges posed by natural products, whose structures were becoming increasingly complex and diverse. In response to these challenges, synthetic organic chemists were prompted to sharpen their art to reach their target molecules, whose structures were often confirmed only after their synthesis in the laboratory through the art and science of total synthesis. The latter became the “locomotive” and the “flagship” of organic synthesis, for through this practice novel synthetic methods were discovered and invented, and also tested for their generality, applicability, and scope with regard to molecular complexity and diversity. The purpose of total synthesis has also evolved over the years to include aspects beyond the synthesis of the molecule and confirmation of its structure. In this article, we briefly review the evolution of total synthesis in terms of its power and reach and demonstrate its current state of the art that combines fundamentals with translational aspects through examples from our laboratories. The highlighted examples reflect the newly emerged paradigm of the discipline that includes—in addition to the total synthesis of the target molecule—structural elucidations, method discovery and development, design, synthesis, and biological evaluation of analogues for biology and medicine, and training of young students, preparing them for academic and industrial careers in the various disciplines that require knowledge and skills to practice the central science of chemical synthesis. Such disciplines include chemical biology, drug discovery and development, materials science and nanotechnology, and other endeavors whose fundamentals depend and rely on the structure of the molecule and its synthesis.

Short Total Synthesis of Δ12-Prostaglandin J2 and Related Prostaglandins. Design, Synthesis, and Biological Evaluation of Macrocyclic Δ12-Prostaglandin J2 Analogues

2018 ◽  
Vol 84 (1) ◽  
pp. 365-378 ◽  
Author(s):  
K. C. Nicolaou ◽  
Kiran Kumar Pulukuri ◽  
Stephan Rigol ◽  
Zisis Peitsinis ◽  
Ruocheng Yu ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Prostaglandin J2

Total Synthesis of Anmindenol A and Its Application to the Design, Synthesis, and Biological Evaluation of Derivatives Thereof

2019 ◽  
Vol 84 (17) ◽  
pp. 10953-10961 ◽  
Author(s):  
Jeyun Jo ◽  
Myeonggyo Jeong ◽  
Ji-Su Ahn ◽  
Jinia Akter ◽  
Hyung-Sik Kim ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of Hybrid Molecules Containing Conjugated Styryl Ketone and α-Bromoacryloyl Moieties

2012 ◽  
Vol 9 (2) ◽  
pp. 140-152 ◽  
Author(s):  
Romeo Romagnoli ◽  
Pier Giovanni Baraldi ◽  
Olga Cruz-Lopez ◽  
Maria Kimatrai Salvador ◽  
Delia Preti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Hybrid Molecules ◽  
Synthesis And Biological Evaluation
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