Books of Interest Calixarenes. An Introduction . By C. David Gutsche . Royal Society of Chemistry , Cambridge, U.K 2008 . xiii + 276 pp. 16 × 24.5 cm. ISBN 9780854042586 . £59.95. Six-Membered Transition States in Organic Synthesis . By Jaemoon  Yang.  Wiley-Interscience,  Hoboken, NJ. 2008. x + 210 pp. 15.5 × 24.5 cm. ISBN 0470178833 . $125.00. Biomarker Methods in Drug Discovery and Development . Edited by Feng  Wang.  Humana Press,  Totowa, NJ. 2008. xviii + 396 pp. 16 × 24 cm. ISBN 978-1-934-11-523-7 . $129.00. Biosimulation in Drug Development . Edited by Martin  Bertau , Erik  Mosekilde , and Hans V.  Westerhoff.  Wiley-VCH,  Weinheim, Germany. 2008. xxviii + 512 pp. 17 × 24.5 cm. ISBN 978-3-527-31699-1 . $215.00. Structure and Reactivity in Organic Chemistry . By Mark G.  Moloney.  Blackwell Publishing, Ltd.,  Oxford, U.K. 2008 . xi + 306 pp. 17 × 24.5 cm. ISBN 1405114517 (Paperback). $55.00. Galectins . Edited by Anatole A.  Klyosov , Zbigniew J.  Witczak , and David  Platt.  Wiley,  Hoboken, NJ.  2008. xi + 279 pp. 16 × 24 cm. ISBN 0470373180 . $110.00.

2008 ◽  
Vol 51 (22) ◽  
pp. 7324-7324
2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Long Li ◽  
Shan Wang ◽  
Pengfei Luo ◽  
Ran Wang ◽  
Zheng Wang ◽  
...  

AbstractSpirocycles play an important role in drug discovery and development. The direct, catalytic, and enantioselective synthesis of spirocycles from readily available starting materials and in an atom economic manner remains a highly sought-after task in organic synthesis. Herein, an enantioselective Pd-hydride-catalyzed cycloaddition method for the synthesis of spirocyclic compounds directly from two classes of commonly available starting materials, 1,3-enynes and cyclic carbon−hydrogen (C−H) bonds, is reported. The reactions employ a chiral Pd/WingPhos catalyst to both suppress the formation of bis-allenyl by-products and control the stereoselectivity. 1,3-Enynes are used as dielectrophilic four-carbon units in the cycloaddition reactions, which also enables an enyne substrate-directed enantioselectivity switch with good levels of stereocontrol. The present spirocycle synthesis tolerates a broad range of functional groups of 1,3-enyne substrates, including alcohols, esters, nitriles, halides, and olefins. A variety of diverse cyclic nucleophiles, including pharmaceutically important heterocycles and carbocycles, can be flexibly incorporated with spiro scaffolds.


Bioanalysis ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 199-201
Author(s):  
Fan Jin ◽  
Daniel Tang ◽  
Kelly Dong ◽  
Dafang Zhong

This article provides an update on new development of China Bioanalysis Forum (CBF). CBF became a member association of Chinese Pharmaceutical Association (CPA) at the end of 2019. The official ceremony and first scientific symposium were held in Shanghai on 18 September 2020. The president of Chinese Pharmaceutical Association and representatives from industry, Contract Research Organization (CRO), hospitals and academic institutes attended the ceremony. Seven experts in the field gave presentations on various topics including Drug Metabolism and Pharmacokinetics (DMPK) and bioanalytical support in drug discovery and development as well as experience in Traditional Chinese Medicine research. With the continuous growth of research and development in China, it is well acknowledged that bioanalysis provides critical support for new innovative medicines and generic drug development in the region.


2019 ◽  
Vol 7 (6) ◽  
pp. 62-67 ◽  
Author(s):  
Amol B Deore ◽  
Jayprabha R Dhumane ◽  
Rushikesh Wagh ◽  
Rushikesh Sonawane

Drug discovery is a process which aims at identifying a compound therapeutically useful in curing and treating disease. This process involves the identification of candidates, synthesis, characterization, validation, optimization, screening and assays for therapeutic efficacy. Once a compound has shown its significance in these investigations, it will initiate the process of drug development earlier to clinical trials. New drug development process must continue through several stages in order to make a medicine that is safe, effective, and has approved all regulatory requirements. One overall theme of our article is that the process is sufficiently long, complex, and expensive so that many biological targets must be considered for every new medicine ultimately approved for clinical use and new research tools may be needed to investigate each new target.  From initial discovery to a marketable medicine is a long, challenging task. It takes about 12 - 15 years from discovery to the approved medicine and requires an investment of about US $1 billion. On an average, a million molecules screened but only a single is explored in late stage clinical trials and is finally made obtainable for patients. This article provides a brief outline of the processes of new drug discovery and development.   


Hematology ◽  
2013 ◽  
Vol 2013 (1) ◽  
pp. 24-29
Author(s):  
Michael R. Grever

Abstract Although enormous progress in therapeutic research has improved the lives of patients with hematologic malignancies, these earlier achievements resulted from strategic combinations of agents with unique mechanisms of action and nonoverlapping toxicities. Continued investment in the modern era of drug discovery and development will focus on targeted therapies. Targeting of specific molecular pathways is expected to achieve effective tumor cell reduction with less overall toxicity. The translational processes involved in moving novel therapeutic strategies from the laboratory toward the clinic require close monitoring. The efforts in both cancer drug discovery and development will require extensive collaboration among basic scientists, clinical investigators, and regulatory scientists. The transition from older methods of therapeutic research will require laboratory support to define eligible patients based upon their pretreatment profile. The principles of preclinical drug development based upon decades of experience in predicting toxicity and designing therapeutic strategies are still needed to insure that safety is a high priority. The opportunities for developing novel targeted combination therapies in uniquely profiled patients will hopefully enable successful breakthroughs. Several concrete examples of exciting new agents are discussed here. Defining the predicted mechanism of resistance to these new targeted agents will enable investigators to subsequently design strategies to circumvent resistance with effective combinations. Drug discovery and development are complex and expensive, so efficiency and cooperation in task completion must be tracked.


2021 ◽  
Author(s):  
Jeffrey D. St. Denis ◽  
Richard J. Hall ◽  
Christopher W. Murray ◽  
Tom D. Heightman ◽  
David C. Rees

Herein is described the concept of fragment sociability and the opportunities for organic chemistry to address the challenges of fragment elaboration.


2020 ◽  
Vol 26 ◽  
Author(s):  
Tadesse Bekele Tafesse ◽  
Mohammed Hussen Bule ◽  
Fazlullah Khan ◽  
Mohammad Abdollahi ◽  
Mohsen Amini

Background: Due to higher failure rates, lengthy time and high cost of the traditional de novo drug discovery and development process; the rate of opportunity to get new, safe and efficacious drugs for the targeted population including pediatric patients with cancer becomes sluggish. Objectives: This paper discusses the development of novel anticancer drugs focusing on the identification and selection of target anticancer drug development for the targeted population. Methods: Information presented in this review was obtained from different databases including PUBMED, SCOPUS, Web of Science, and EMBASE. Various keywords were used as search terms. Results: The pharmaceutical companies currently are executing drug repurposing as an alternative means to accelerate the drug development process that reduces the risk of failure, time and cost, which takes 3-12 years with almost 25% overall probability of success as compared to de novo drug discovery and development process (10-17 years) which has less than 10% probability of success. An alternative strategy to the traditional de novo drug discovery and development process, called drug repurposing, is also presented. Conclusion: Therefore, to continue with the progress of developing novel anticancer drugs towards the targeted population, identification and selection of the target to the specific disease type is important considering the aspects of the age of the patient and the disease stages such as each cancer types are different when we consider the disease at a molecular level. Drug repurposing technique becomes an influential alternative strategy to discover and develop novel anticancer drug candidates.


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