scholarly journals Synthesis and pre-clinical evaluation of a [18F]fluoromethyl-tanaproget derivative for imaging of progesterone receptor expression

RSC Advances ◽  
2016 ◽  
Vol 6 (62) ◽  
pp. 57569-57579 ◽  
Author(s):  
Shairoz Merchant ◽  
Louis Allott ◽  
Laurence Carroll ◽  
Vickram Tittrea ◽  
Steven Kealey ◽  
...  
Keyword(s):  
Progesterone Receptor ◽  
Clinical Evaluation ◽  
Biological Evaluation ◽  
Receptor Expression ◽  
Progesterone Receptor Expression ◽  
High Affinity ◽  
Synthesis And Biological Evaluation

This work features the synthesis and biological evaluation of a novel fluorinated derivative of tanaproget and a carbon-11 labelled analogue, a high affinity non-steroidal PR ligand, as a possible candidate for imaging PR expressionin vivo.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

scholarly journals Sex-specific modification of progesterone receptor expression by 17β-oestradiol in human cardiac tissues

2010 ◽  
Vol 1 (1) ◽  
pp. 2 ◽  
Author(s):  
Georgios Kararigas ◽  
Eva Becher ◽  
Shokoufeh Mahmoodzadeh ◽  
Christoph Knosalla ◽  
Roland Hetzer ◽  
...  
Keyword(s):  
Progesterone Receptor ◽  
Receptor Expression ◽  
Progesterone Receptor Expression ◽  
Cardiac Tissues ◽  
Specific Modification

Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

2017 ◽  
Vol 46 (21) ◽  
pp. 7005-7019 ◽  
Author(s):  
Benjamin W. J. Harper ◽  
Emanuele Petruzzella ◽  
Roman Sirota ◽  
Fernanda Fabiola Faccioli ◽  
Janice R. Aldrich-Wright ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

Synthesis and biological evaluation of mixed-ligands cyclometalated iridium(III)-quinoline complexes

2021 ◽  
Author(s):  
Yan Yang ◽  
Cheng-Ming Wang ◽  
Feng-Hua Pan ◽  
Qi-Pin Qin ◽  
Qiu-Ji Xie ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
In Vivo Efficacy ◽  
Mixed Ligands ◽  
Synthesis And Biological Evaluation ◽  
Insight Into

With the aim of gaining new insight into the underlying apoptosis mechanisms and in vivo efficacy of cyclometalated Ir(III) complexes as metalodrugs, six new cyclometalated Ir(III)-quinoline complexes, [Ir(1a)(2pq)2] (2a), [Ir(1b)(2pq)2]...

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