Oxazole: A Promising Building Block for the Development of Potent Antitumor Agents

2016 ◽  
Vol 16 (30) ◽  
pp. 3582-3589 ◽  
Author(s):  
Hua Zhou ◽  
Jiang-Qun Cheng ◽  
Zhi-Sen Wang ◽  
Fei-Hu Chen ◽  
Xin-Hua Liu
Keyword(s):  
Building Block ◽  
Antitumor Agents

Microbe Engineering of Guaia-6,10(14)-diene as a Building Block for the Semisynthetic Production of Plant-Derived (−)-Englerin A

2019 ◽  
Author(s):  
Thomas Siemon ◽  
Zhangqian Wang ◽  
Guangkai Bian ◽  
Tobias Seitz ◽  
Ziling Ye ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Saccharomyces Cerevisiae ◽  
Synthetic Biology ◽  
Chemical Synthesis ◽  
Building Block ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Economical Method ◽  
Englerin A ◽  
Transient Receptor

Herein, we report the semisynthetic production of the potent transient receptor potential canonical (TRPC) channel agonist (−)-englerin A (EA), using guaia-6,10(14)-diene as the starting material. Guaia-6,10(14)-diene was systematically engineered in Escherichia coli and Saccharomyces cerevisiae using the CRISPR/Cas9 system and produced with high titers. This provided us the opportunity to execute a concise chemical synthesis of EA and the two related guaianes (−)-oxyphyllol and (+)-orientalol E. The potentially scalable approach combines the advantages of synthetic biology and chemical synthesis and provides an efficient and economical method for producing EA as well as its analogs.

Microbe Engineering of Guaia-6,10(14)-diene as a Building Block for the Semisynthetic Production of Plant-Derived (−)-Englerin A

2019 ◽  
Author(s):  
Thomas Siemon ◽  
Zhangqian Wang ◽  
Guangkai Bian ◽  
Tobias Seitz ◽  
Ziling Ye ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Saccharomyces Cerevisiae ◽  
Synthetic Biology ◽  
Chemical Synthesis ◽  
Building Block ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Economical Method ◽  
Englerin A ◽  
Transient Receptor

Herein, we report the semisynthetic production of the potent transient receptor potential canonical (TRPC) channel agonist (−)-englerin A (EA), using guaia-6,10(14)-diene as the starting material. Guaia-6,10(14)-diene was systematically engineered in Escherichia coli and Saccharomyces cerevisiae using the CRISPR/Cas9 system and produced with high titers. This provided us the opportunity to execute a concise chemical synthesis of EA and the two related guaianes (−)-oxyphyllol and (+)-orientalol E. The potentially scalable approach combines the advantages of synthetic biology and chemical synthesis and provides an efficient and economical method for producing EA as well as its analogs.

Ultrastrong, Free-Standing and Large Nanofilms of Pyrenearamid

2019 ◽  
Author(s):  
Amalia Rapakousiou ◽  
Alejandro López-moreno ◽  
Belén Nieto-Ortega ◽  
M. Mar Bernal ◽  
Miguel A. Monclús ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Building Block ◽  
Aromatic Polyamide ◽  
Free Standing ◽  
Spatial Confinement ◽  
Polymeric Structure ◽  
Reduced Modulus ◽  
Organizational Arrangement ◽  
Polycyclic Aromatic ◽  
Nanoscale Building Block

We introduce poly(1,6-pyrene terephthalamide) polymer (PPyrTA) as an aromatic polyamide analogue of poly(p-phenylene terephthalamide) (PPTA), also known as Kevlar®. This work shows that the incorporation of polycyclic aromatic pyrene moieties improves drastically the mechanical properties of the polymeric structure, increasing elastic nanoindentation-determined modulus and hardness by factors of 1.9 and 4.3, respectively. Liquid deprotonated dispersions of PPyrTA nanofibers were used as nanoscale building block for producing large-surface, free-standing polymer macroscopic nanofilms. This 2D assembly leads to further significant improvements in reduced modulus and hardness (more than twice) compared to the starting polymer macroscale fibres, due to a better re-organizational arrangement of the PPyrTA nanofibers in the nanofilms, formed under 2D spatial confinement.

Thienopyrrolocarbazoles: New Building Blocks for Functional Organic Materials

2019 ◽  
Author(s):  
Dorian Bader ◽  
Johannes Fröhlich ◽  
Paul Kautny
Keyword(s):  
Building Block ◽  
Organic Materials ◽  
Building Blocks ◽  
Molecular Properties ◽  
The Family ◽  
Facile Preparation

The facile preparation of three regioisomeric thienopyrrolocarbazoles applying a convenient C-H activation approach is presented. Derived from indolo[3,2,1-<i>jk</i>]carbazole, the incorporation of thiophene into the triarylamine framework significantly impacted the molecular properties of the parent scaffold. The developed thienopyrrolocarbazoles enrich the family of triarylamine donors and constitute a novel building block for functional organic materials.

Thienopyrrolocarbazoles: New Building Blocks for Functional Organic Materials

2019 ◽  
Author(s):  
Dorian Bader ◽  
Johannes Fröhlich ◽  
Paul Kautny
Keyword(s):  
Building Block ◽  
Organic Materials ◽  
Building Blocks ◽  
Molecular Properties ◽  
The Family ◽  
Facile Preparation

The facile preparation of three regioisomeric thienopyrrolocarbazoles applying a convenient C-H activation approach is presented. Derived from indolo[3,2,1-<i>jk</i>]carbazole, the incorporation of thiophene into the triarylamine framework significantly impacted the molecular properties of the parent scaffold. The developed thienopyrrolocarbazoles enrich the family of triarylamine donors and constitute a novel building block for functional organic materials.

Vitamin D as potential therapeutic anticancer agent

2018 ◽  
pp. 1-3
Keyword(s):  
Vitamin D ◽  
Anticancer Activity ◽  
Anticancer Agent ◽  
Antitumor Agents ◽  
Metastatic Potential ◽  
Anticancer Properties ◽  
Chemotherapy Agents

The role of vitamin D is implicated in carcinogenesis through numerous biological processes like induction of apoptosis, modulation of immune system inhibition of inflammation and cell proliferation and promotion of cell differentiation. Its use as additional adjuvant drug with cancer treatment may be novel combination for improved outcome of different cancers. Numerous preclinical, epidemiological and clinical studies support the role of vitamin D as an anticancer agent. Anticancer properties of vitamin D have been studied widely (both in vivo and in vitro) among various cancers and found to have promising results. There are considerable data that indicate synergistic potential of calcitriol and antitumor agents. Possible mechanisms for modulatory anticancer activity of vitamin D include its antiproliferative, prodifferentiating, and anti-angiogenic and apoptic properties. Calcitriol reduces invasiveness and metastatic potential of many cancer cells by inhibiting angiogenesis and regulating expression of the key molecules involved in invasion and metastasis. Anticancer activity of vitamin D is synergistic or additive with the antineoplastic actions of several drugs including cytotoxic chemotherapy agents like paclitaxel, docetaxel, platinum base compounds and mitoxantrone. Benefits of addition of vitamin D should be weighed against the risk of its toxicity.

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