NDLI: The use of isolated natural products as scaffolds for the generation of chemically diverse screening libraries for drug discovery.

Please wait, while we are loading the content...

Year: 2017 Volume: 34

Year: 2016 Volume: 33

Year: 2016 Volume: 33 Issue: 10

Year: 2016 Volume: 33 Issue: 9

Year: 2016 Volume: 33 Issue: 8

Year: 2016 Volume: 33 Issue: 7

Year: 2016 Volume: 33 Issue: 6

Year: 2016 Volume: 33 Issue: 5

Year: 2016 Volume: 33 Issue: 4

Year: 2016 Volume: 33 Issue: 3

Synthetic approaches towards alkaloids bearing -tertiary amines.

Fragmentation reactions using electrospray ionization mass spectrometry: an important tool for the structural elucidation and characterization of synthetic and natural products.

The chemistry and biology of guanidine natural products.

The use of isolated natural products as scaffolds for the generation of chemically diverse screening libraries for drug discovery.

Marine natural products.

Year: 2016 Volume: 33 Issue: 2

Year: 2016 Volume: 33 Issue: 1

Year: 2015 Volume: 32

Year: 2014 Volume: 31

Year: 2013 Volume: 30

Year: 2012 Volume: 29

Year: 2011 Volume: 28

Year: 2010 Volume: 27

Year: 2009 Volume: 26

The use of isolated natural products as scaffolds for the generation of chemically diverse screening libraries for drug discovery.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Barnes, Emma C. Kumar, Rohitesh Davis, Rohan A.
Description	Country affiliation: Australia Author Affiliation: Barnes EC ( Eskitis Institute for Drug Discovery, Griffith University, Brisbane, QLD 4111, Australia. r.davis@griffith.edu.au.)
Abstract	A diverse range of strategies leading to natural product derived or inspired screening libraries aims to increase the number of new chemical entities emerging per year. However, the use of isolated natural products as scaffolds for the semi-synthesis of larger biological screening libraries remains rare. This particular method avoids the time-consuming and resource intensive de novo synthetic strategy for scaffold production, and has become more feasible through improvements to synthetic and isolation methodologies. This Highlight examines the increasing popularity of small- to large-sized screening libraries generated directly from isolated natural products. Several of the examples detailed herein show how this strategy can lead to improvements in not only potency but also other important (and often forgotten) drug discovery parameters such as toxicity, selectivity, lipophilicity and bioavailability. However, there are still improvements to be made to this method, particularly in the choice of the natural product scaffold and the derivatising reagents used. Avoidance of known nuisance compounds or structural alert motifs (e.g. PAINS) that interfere with bioactivity screens, and impact downstream drug development will play a significant role in the future success of this methodology. Incorporation of rational design strategies that take into account the physicochemical parameters (e.g. log P, MW, HBA, HBD) of the final semi-synthetic library analogues will also facilitate the discovery and development of leads and drugs. A multi-pronged approach to drug discovery that incorporates the use of isolated natural product scaffolds for library generation will surely be beneficial.
File Format	HTM / HTML
ISSN	02650568
Issue Number	3
Journal	Natural Product Reports
Volume Number	33
e-ISSN	14604752
Language	English
Publisher	Royal Society of Chemistry
Publisher Date	2016-03-01
Publisher Place	Great Britain (UK)
Access Restriction	Subscribed
Subject Keyword	Discipline Chemistry Biological Products Chemistry Drug Discovery Molecular Structure Small Molecule Libraries Journal Article Research Support, Non-u.s. Gov't Review
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Drug Discovery Biochemistry

Central Library (ISO-9001:2015 Certified)
Indian Institute of Technology Kharagpur
Kharagpur, West Bengal, India | PIN - 721302

See location in the Map
03222 282435
Mail: support@ndl.gov.in

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in