Synthesis, Proteolytic Stability, and In vitro Evaluation of DOTA Conjugated p160 Peptide Based Radioconjugates: [177Lu]Lu-DOTA-p160

2021 ◽  
Author(s):  
Jasleen Kaur ◽  
Karim Arroub ◽  
Alexander Drzezga ◽  
Klaus Schomaecker ◽  
Sanjay Mathur
Keyword(s):  
Biological Evaluation ◽  
In Vitro Evaluation ◽  
Enzymatic Stability ◽  
Proteolytic Stability ◽  
In Vitro Stability

In this work, we describe the synthesis, in-vitro stability, and preliminary biological evaluation of [177Lu]Lu-DOTA-p160 peptide-based radiopharmaceuticals. Our findings highlight that all DOTA-p160-peptide radioconjugates exhibit favorable proteolytic and enzymatic stability...

scholarly journals Design, Synthesis, and In Vitro Evaluation of Benzofuro[3,2-c]Quinoline Derivatives as Potential Antileukemia Agents

Molecules ◽  
2020 ◽  
Vol 25 (1) ◽  
pp. 203 ◽  
Author(s):  
Ying Lin ◽  
Dong Xing ◽  
Wen-Biao Wu ◽  
Gao-Ya Xu ◽  
Li-Fang Yu ◽  
...  
Keyword(s):  
Intramolecular Cyclization ◽  
Biological Evaluation ◽  
Quinoline Derivatives ◽  
Reaction Conditions ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Metal Free ◽  
Sequential Transformation ◽  
High Yields

Herein, we design and synthesize an array of benzofuro[3,2-c]quinolines starting from 3-(2-methoxyphenyl)quinolin-4(1H)ones via a sequential chlorination/demethylation, intramolecular cyclization pathway. This sequential transformation was efficient, conducted under metal-free and mild reaction conditions, and yielded corresponding benzofuro[3,2-c]quinolines in high yields. In vitro biological evaluation indicated that such type of compounds showed excellent antileukemia activity and selectivity, and therefore may offer a promising hit compound for developing antileukemia compounds.

Ester Prodrugs of Ketoprofen: Synthesis, In Vitro Stability, In Vivo Biological Evaluation and In Silico Comparative Docking Studies Against COX-1 and COX-2

2016 ◽  
Vol 13 (1) ◽  
pp. 41-57 ◽  
Author(s):  
Musa Ahmed ◽  
Faizul Azam ◽  
Abdul Gbaj ◽  
Abdulmottaleb E. Zetrini ◽  
Amna S. Abodlal ◽  
...  
Keyword(s):  
In Silico ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Cox 2 ◽  
In Vitro Stability ◽  
Ester Prodrugs ◽  
Cox 1

In vitro evaluation of IL-18 effects in Crohn's disease

2001 ◽  
Vol 120 (5) ◽  
pp. A316-A317
Author(s):  
P MAERTEN ◽  
S COLPAERT ◽  
Z LIU ◽  
K GEBOES ◽  
J CEUPPENS ◽  
...  
Keyword(s):  
Crohn’S Disease ◽  
Crohn's Disease ◽  
In Vitro Evaluation

52: In Vitro Evaluation of Ureteral Stent Compression

2006 ◽  
Vol 175 (4S) ◽  
pp. 18-18
Author(s):  
Kari Hendlin ◽  
Krishna Vedula ◽  
Christina Horn ◽  
Manoj Monga
Keyword(s):  
Ureteral Stent ◽  
In Vitro Evaluation

Purification hemisynthesis of xanthatin derivates and in vitro evaluation of their activity towards farnesyltransferase (PFTase)

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
B Pinel ◽  
A Landreau ◽  
J Dubois ◽  
G Au do ◽  
F De la Poype ◽  
...  
Keyword(s):  
In Vitro Evaluation

In vitro evaluation of the effect of selected herbal extracts on drug transport across porcine jejunal tissue

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
C Tarirai ◽  
A Viljoen ◽  
P Chinyemba ◽  
A Khatib ◽  
P Jiyane ◽  
...  
Keyword(s):  
Drug Transport ◽  
Herbal Extracts ◽  
In Vitro Evaluation

In vitro evaluation of the synergetic interaction between antibiotics tetracyclin and penicillin with (+)-usnic acid isolated from Usnea steineri against multiresistant bacteria

Planta Medica ◽  
2014 ◽  
Vol 80 (16) ◽  
Author(s):  
M Gomide Tozatti ◽  
D da Silva Ferreira ◽  
G Morette Mazza ◽  
T da Silva Moraes ◽  
CH Gomes Martins ◽  
...  
Keyword(s):  
Usnic Acid ◽  
In Vitro Evaluation ◽  
Multiresistant Bacteria
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