Design, Synthesis, and Biological Evaluation of Fluoroneplanocin A as the Novel Mechanism-Based Inhibitor ofS-Adenosylhomocysteine Hydrolase

2003 ◽  
Vol 46 (2) ◽  
pp. 201-203 ◽  
Author(s):  
Lak Shin Jeong ◽  
Su Jeong Yoo ◽  
Kang Man Lee ◽  
Mi Jeong Koo ◽  
Won Jun Choi ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
The Novel ◽  
Design Synthesis ◽  
Adenosylhomocysteine Hydrolase ◽  
Synthesis And Biological Evaluation

Design, Synthesis and Biological Evaluation of the Novel Antitumor Agent Aurone Derivatives

2013 ◽  
Vol 781-784 ◽  
pp. 1235-1239
Author(s):  
Qian Nan Guo ◽  
Lei Lv ◽  
Yao Zhou ◽  
Peng Yu ◽  
Yuou Teng
Keyword(s):  
Biological Activities ◽  
Antitumor Agent ◽  
Biological Evaluation ◽  
The Novel ◽  
Pharmacological Activities ◽  
Design Synthesis ◽  
H Nmr ◽  
Wide Range ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation

Aurones belong to a class of heterocyclic flavonoids which contains a benzofuran element associated with a benzylidene linked in position 2. Aurones possess a wide range of pharmacological activities and biological activities, such as antitumor, antifungal, phytoalexin and so on. A novel series of 2-ayl-yl (5-methacrylate) aurone analogues were synthesized in six steps with the overall yield of 11%-13% and characterized by 1H NMR. Among the key intermediates and target compounds, 2-(2-furan-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7a) and 2-(2-thienyl-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7b) have never been reported before. Primary biological activities evaluation showed that 7a exhibited good inhibitory activities against K562 with an IC50 of 2.18 μM and against HepG2 with an IC50 of 3.95μM.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Thiazolidinone Derivatives

2021 ◽  
Vol 33 (10) ◽  
pp. 2379-2385
Author(s):  
Reshma Sathyanarayana ◽  
Boja Poojary ◽  
B. Sukesh Kumar ◽  
Vasantha Kumar ◽  
Rajesh P. Shastry ◽  
...  
Keyword(s):  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
The Novel ◽  
Design Synthesis ◽  
Scavenging Effect ◽  
Elemental Analyses ◽  
Radical Scavenging Effect ◽  
Ft Ir ◽  
Synthesis And Biological Evaluation

In present study, the novel thiazolidinone derivatives were designed and synthesized. The formation of the target compounds was confirmed by the elemental analyses, FT-IR, mass spectroscopy and 1H NMR spectroscopy. These derivatives were subjected to antibacterial and antioxidant activities. The antibacterial results revealed that these derivatives were selectively active against Gram-negative Pseudomonas aeruginosa bacteria. Also, these derivatives displayed a good DPPH radical scavenging effect. Drosophila melanogaster flies were used for evaluating the toxic impact of novel thiazolidinone derivatives.

The design, synthesis and biological evaluation of novel thiamin diphosphate analog inhibitors against the pyruvate dehydrogenase multienzyme complex E1 from Escherichia coli

2014 ◽  
Vol 12 (44) ◽  
pp. 8911-8918 ◽  
Author(s):  
Lingling Feng ◽  
Junbo He ◽  
Haifeng He ◽  
Lulu Zhao ◽  
Lingfu Deng ◽  
...  
Keyword(s):  
Pyruvate Dehydrogenase ◽  
Potent Inhibitor ◽  
Binding Mode ◽  
Biological Evaluation ◽  
The Novel ◽  
Multienzyme Complex ◽  
Thiamin Diphosphate ◽  
Design Synthesis ◽  
E Coli ◽  
Synthesis And Biological Evaluation

Optimal binding mode for the novel potent inhibitor 4j against PDHc-E1 from E. coli.

scholarly journals Novel unit B cryptophycin analogues as payloads for targeted therapy

2018 ◽  
Vol 14 ◽  
pp. 1281-1286 ◽  
Author(s):  
Eduard Figueras ◽  
Adina Borbély ◽  
Mohamed Ismail ◽  
Marcel Frese ◽  
Norbert Sewald
Keyword(s):  
Targeted Therapy ◽  
Triethylene Glycol ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
The Novel ◽  
Design Synthesis ◽  
Naturally Occurring ◽  
Synthesis And Biological Evaluation ◽  
Hydroxyethyl Group

Cryptophycins are naturally occurring cytotoxins with great potential for chemotherapy. Since targeted therapy provides new perspectives for treatment of cancer, new potent analogues of cytotoxic agents containing functional groups for conjugation to homing devices are required. We describe the design, synthesis and biological evaluation of three new unit B cryptophycin analogues. The O-methyl group of the unit B D-tyrosine analogue was replaced by an O-(allyloxyethyl) moiety, an O-(hydroxyethyl) group, or an O-(((azidoethoxy)ethoxy)ethoyxethyl) substituent. While the former two maintain cytotoxicity in the subnanomolar range, the attachment of the triethylene glycol spacer with a terminal azide results in a complete loss of activity. Docking studies of the novel cryptophycin analogues to β-tubulin provided a rationale for the observed cytotoxicities.

Sign in / Sign up

Export Citation Format

Share Document