Design and Synthesis of 12-Aza-Epothilones (Azathilones)—“Non-Natural” Natural Products with Potent Anticancer Activity

2006 ◽  
Vol 45 (35) ◽  
pp. 5880-5885 ◽  
Author(s):  
Fabian Feyen ◽  
Jürg Gertsch ◽  
Markus Wartmann ◽  
Karl-Heinz Altmann
Keyword(s):  
Natural Products ◽  
Anticancer Activity ◽  
Design And Synthesis

Design and synthesis of a hybrid framework of indanone and chromane: total synthesis of a homoisoflavanoid, brazilane

2018 ◽  
Vol 16 (1) ◽  
pp. 89-100 ◽  
Author(s):  
Jinwoo Kim ◽  
Ikyon Kim
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Hybrid Structure ◽  
Design And Synthesis ◽  
Hybrid Framework

A chemical backbone of tetracyclic homoisoflavanoid natural products such as brazilin inspired us to design a new chemical scaffold, 6a,11b-dihydroindeno[2,1-c]chromen-7(6H)-one, which is a hybrid structure of indanone and chromane.

Design and synthesis of 21-alkynylaryl pregnenolone derivatives and evaluation of their anticancer activity

2014 ◽  
Vol 22 (24) ◽  
pp. 6980-6988 ◽  
Author(s):  
György Szalóki ◽  
Athanasia Pantzou ◽  
Kyriakos C. Prousis ◽  
Olga Mavrofrydi ◽  
Panagiota Papazafiri ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Design And Synthesis

Synthesis of the 10-oxabicyclo[5.2.1]decane framework present in bioactive natural products

2018 ◽  
Vol 16 (9) ◽  
pp. 1557-1580 ◽  
Author(s):  
Ángel M. Montaña ◽  
Stefano Ponzano ◽  
Maria-Filomena Sanasi ◽  
Gabriele Kociok-Köhn
Keyword(s):  
Natural Products ◽  
Anticancer Activity ◽  
Synthetic Method ◽  
Bioactive Natural Products

Development of a versatile and scalable synthetic method of the 10-oxabicyclo[5.2.1]decane framework present in bioactive natural products. The evaluation of the anticancer activity of the synthesized compounds against leukaemia showed a promising activity.

scholarly journals Synthetic Approaches to Tetracyclic Pyrrole Imidazole Marine Alkaloids

2013 ◽  
Vol 8 (7) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Takuya Imaoka ◽  
Makoto Iwata ◽  
Takafumi Akimoto ◽  
Kazuo Nagasawa
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Anticancer Activity ◽  
Biological Activities ◽  
Structural Complexity ◽  
Marine Alkaloids ◽  
Ring Systems ◽  
Agonistic Activity ◽  
Synthetic Approaches

Oroidin derived pyrrole imidazole marine alkaloids (PIAs) are attractive targets for synthetic organic chemists because of their structural complexity and diversity as well as their interesting biological activities. A number of efforts have been carried out to develop strategies for the synthesis of these natural products. Members of PIAs ( eg., 2-7) which contain tetracyclic ring systems possessing characteristic cyclic guanidine or urea moieties show significant biological activities including anticancer activity and agonistic activity against the adrenoceptor. In this review investigations of the total synthesis of the representative tetracyclic PIAs dibromophakellin (2) and dibromophakellstatin (3) are described.

Structure-based synthesis: From natural products to drug prototypes

2009 ◽  
Vol 81 (6) ◽  
pp. 1085-1091 ◽  
Author(s):  
Stephen Hanessian
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Design Element ◽  
X Ray ◽  
Design And Synthesis ◽  
Highly Active ◽  
In Vitro Inhibition ◽  
Inhibitory Activities ◽  
Active Natural

X-ray crystallographic data available from complexes of natural and synthetic molecules with the enzyme thrombin has led to the design and synthesis of truncated and hydrid molecules exhibiting excellent inhibition in vitro. The design element has also been extended to the synthesis and in vitro inhibition of a series of achiral molecules deploying aromatic and heterocyclic core motifs with appropriately functionalized appendages that provide excellent binding interactions at the S1, S2, and S3 sites of thrombin. Excellent selectivity for thrombin over trypsin has also been observed. Thus, studies in total synthesis of highly active natural aeruginosins have inspired further work toward truncated and hybrid analogs with excellent inhibitory activities. Structure-based organic synthesis has guided our research from natural products toward unnatural drug-like prototypes.

Mechanism-Guided Design and Synthesis of a Mitochondria-Targeting Artemisinin Analogue with Enhanced Anticancer Activity

2016 ◽  
Vol 128 (44) ◽  
pp. 13974-13978 ◽  
Author(s):  
Chong-Jing Zhang ◽  
Jigang Wang ◽  
Jianbin Zhang ◽  
Yew Mun Lee ◽  
Guangxue Feng ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Design And Synthesis ◽  
Mitochondria Targeting
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