Radiolabeled farnesyl-protein transferase inhibitors

The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in compe...

Burns, Donald H.，Hamill, Terence G.，RE Gibson - WO

Potent and selective farnesyl transferase inhibitors.

We recently described a novel series of CA(1)A(2)X peptidomimetics as farnesyl transferase inhibitors (FTIs). These compounds possess an N-(4-piperidinyl)b...

R Millet，J Domarkas，R Houssin，... - 《Journal of Medicinal Chemistry》

Potent and Selective Farnesyl Transferase Inhibitors

We recently described a novel series of CA 1 A 2 X peptidomimetics as farnesyl transferase inhibitors (FTIs). These compounds possess an N -(4-piperidinyl)benzamide scaffold mimicking A 1 A 2 residue. Extensive exploration of structurea...

TL Diguarher，JC Ortuno，D Shanks，...

Inhibitors of Protein: Geranylgeranyl Transferases.

The enzyme protein:geranylgeranyl transferase-1 (PGGT-1 or GGTase-I) catalyzes the geranylgeranylation of cysteine residues near the C-termini of a variety...

E Oualid，Farid，Cohen，... - 《Current Medicinal Chemistry》

Macrocyclic Piperazinones as Potent Dual Inhibitors of Farnesyltransferase and Geranylgeranyltransferase-I.

For Abstract see ChemInform Abstract in Full Text.

CJ Dinsmore，EAE Al. - 《Cheminform》

Macrocyclic Piperazinones as Potent Dual Inhibitors of Farnesyltransferase and Geranylgeranyltransferase㊣.

For Abstract see ChemInform Abstract in Full Text.

CJ Dinsmore，EAE Al. - 《Cheminform》

作用于FTase和Raf-1激酶的新型抗肿瘤药物的设计

Ras/Raf/MEK/ERK信号通路,在肿瘤细胞的增殖,分化,凋亡,转移,代谢等过程中起着重要的作用,本文着眼于Ras/Raf/MEK/ERK信号通路中的关键靶点,以法尼基转移酶(FTase)为主...

赵娟，朱一婧，曾露，... - 《药学学报》

1,4-Diaryl-2-mercaptoimidazoles derivatives as a novel class of antimicrobial agents: design, synthesis, and computational studies

In search of a new class of potential antimicrobial agents, some 1,4-diaryl-2-mercaptoimidazoles (5a–5h) were prepared by employing a mild and green appro...

GK Gupta，V Saini，R Khare，... - 《Medicinal Chemistry Research》

Synthesis and Cytotoxicity Evaluation of Some Novel 1-(3-Chlorophenyl) piperazin-2-one Derivatives Bearing Imidazole Bioisosteres

A series of substituted 3-chlorophenylpiperazinone derivatives were synthesised using L-778123 (an imidazole-containing FTase inhibitor) as a model by bioi...

S Ghasemi，S Sharifi，S Davaran，... - 《Australian Journal of Chemistry》

Indispensability of Imidazole Moiety in new drug development-A Review

The significance of imidazole heterocyclic nucleus in new drug development is worth mentioning. The wide range of its applica- tion has drawn an immense at...

N Mohammad，N Srivastava，B Yogi，...