Literature

Abstract

A series of novel N(3/8)-disubstituted-3,8-diazabicyclo[3.2.1]octanes in order to improve the in vitro activity of the prototype 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridyl-4-yl)methylpiperazine (1) were synthesized and evaluated by assays of growth inhibition against several tumor cell lines. Compounds 2a,b,f and m demonstrated not only growth-inhibitory activities against leukemia cancer cells, but also fairly good activities against the growth of certain solid tumors. Among them, 2a is the most potent one with IC(50) values in the low micromolar range. Moreover, compound 2a has been selected for in vitro testing on MCF-7 cell to evaluate the mode of action of this lead compound.

DOI： 10.1016/j.ejmech.2006.11.013

Synthesis and antiproliferative properties of N3/8-disubstituted 3,8-diazabicyclo[3.2.1]octane analogues of 3,8-bis[2-(3,4,5-trimethoxyphenyl)pyridin-4-yl]methyl-piperazine

European Journal of Medicinal Chemistry 2007.0

Synthesis and antiproliferative activity of 4-substituted-piperazine-1-carbodithioate derivatives of 2,4-diaminoquinazoline

European Journal of Medicinal Chemistry 2013.0

Design and synthesis of 3,5-dialkylamino substituted 8H,10H-3(R),5(R),15b(S)-2,3,6,7-tetrahydro-1,5,3-dioxazepino[3,2-c]indolo[3,2-g]pteridine-7-ones

Bioorganic & Medicinal Chemistry Letters 1997.0

Novel benzothiazine-piperazine derivatives by peptide-coupling as potential anti-proliferative agents

Bioorganic & Medicinal Chemistry Letters 2017.0

One-pot synthesis and antiproliferative activity of novel 2,4-diaminopyrimidine derivatives bearing piperidine and piperazine moieties

European Journal of Medicinal Chemistry 2014.0

The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1] octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones