Cytochalasins from an Australian Marine Sediment-Derived Phomopsis sp. (CMB-M0042F): Acid-Mediated Intramolecular Cycloadditions Enhance Chemical Diversity

2017 ◽  
Vol 82 (18) ◽  
pp. 9704-9709 ◽  
Author(s):  
Zhuo Shang ◽  
Ritesh Raju ◽  
Angela A. Salim ◽  
Zeinab G. Khalil ◽  
Robert J. Capon
Keyword(s):  
Marine Sediment ◽  
Chemical Diversity ◽  
Intramolecular Cycloadditions

What can phylogeny tell us about chemical diversity?

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
N Rønsted ◽  
GI Stafford ◽  
AW Meerow ◽  
G Petersen ◽  
J Van Staden ◽  
...  
Keyword(s):  
Chemical Diversity

High throughput screening to investigate Brazilian Cerrado biome plant extract bank chemical diversity

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
LS Espindola ◽  
RG Dusi ◽  
KR Gustafson ◽  
J McMahon ◽  
JA Beutler
Keyword(s):  
High Throughput ◽  
Plant Extract ◽  
High Throughput Screening ◽  
Chemical Diversity ◽  
Brazilian Cerrado ◽  
Cerrado Biome

Rapid Elaboration of Fragments into Leads Applied to Bromodomain-3 Extra Terminal Domain

2020 ◽  
Author(s):  
Luke Adams ◽  
Lorna E. Wilkinson-White ◽  
Menachem J. Gunzburg ◽  
Stephen J. Headey ◽  
Martin J. Scanlon ◽  
...  
Keyword(s):  
Binding Site ◽  
Systematic Approach ◽  
Structural Information ◽  
Peptide Binding ◽  
Chemical Diversity ◽  
Chemical Probes ◽  
Protein Targets ◽  
Structure Activity ◽  
Peptide Binding Site ◽  
Selection Of

The development of low-affinity fragment hits into higher affinity leads is a major hurdle in fragment-based drug design. Here we demonstrate an approach for the Rapid Elaboration of Fragments into Leads (REFiL) applying an integrated workflow that provides a systematic approach to generate higher-affinity binders without the need for structural information. The workflow involves the selection of commercial analogues of fragment hits to generate preliminary structure-activity relationships. This is followed by parallel microscale chemistry using chemoinformatically designed reagent libraries to rapidly explore chemical diversity. Upon completion of a fragment screen against Bromodomain-3 extra terminal (BRD3-ET) domain we applied the REFiL workflow, which allowed us to develop a series of tetrahydrocarbazole ligands that bind to the peptide binding site of BRD3-ET. With REFiL we were able to rapidly improve binding affinity >30-fold. The REFiL workflow can be applied readily to a broad range of protein targets without the need of a structure, allowing the efficient evolution of low-affinity fragments into higher affinity leads and chemical probes.<br>

An assessment of toxic metals content in the marine sediments of the Shuaiba Industrial Area, Kuwait, after the oil spill during the Gulf War

1996 ◽  
Vol 34 (7-8) ◽  
pp. 203-210 ◽  
Author(s):  
S. Al-Muzaini ◽  
P. G. Jacob
Keyword(s):  
Oil Spill ◽  
Marine Sediment ◽  
Oil Spills ◽  
Industrial Area ◽  
Gulf War ◽  
Oil Wells ◽  
Environmental Damage ◽  
Base Line ◽  
Sampling Locations ◽  
Very High

A field study was carried out involving seven fixed sampling stations. The sampling locations were selected to cover the distribution of pollutants in the Shuaiba Industrial Area (SIA), which was contaminated with oil released from oil wells and broken pipelines and with a vast amount of burnt and unburnt crude oil from the burning and gushing oil wells. The samples were collected biweekly between July 1993 and July 1994. The concentrations of V, Ni, Cr, Cd and Pb were determined and compared with the previously collected baseline data to assess the degree of environmental damage caused due to the oil spills during the Gulf war. The average concentrations (mg/kg) of various elements in the marine sediment were 17.3 for V, 30.8 for Ni, 55.5 for Cr, 0.02 for Cd and 1.95 for Pb. Our results show that even after the heavy spillage of oil, associated metal concentrations were not very high compared with previously reported base line values.

Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

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