Protein Information

Name integrin
Synonyms Alpha 11 precursor; HsT18964; ITGA11; Integrin; Integrin alpha 11; Integrin alpha 11 precursor; MSTP018; HsT18964s…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
19545055 Cheng GY, Ni GH, Jiang FC: [Pharmacophore model of integrin alphavbeta3 antagonists] . Yao Xue Xue Bao. 2009 Apr;44(4):379-85.

Thirty compounds (four categories) with highly inhibitory activity against the integrin alphavbeta3 receptor (IC50 < 110 nmol x L (-1)), amide, piperazine, piperidine, gamma-valerolactam as the intermediate junction, separately, were selected as a training set to construct a three-dimensional pharmacophore models of integrin alphavbeta3 receptor antagonists with the Catalyst software.
84(1,1,1,4) Details
20067886 Poplawska B, Bielawska A, Surazynski A, Czarnomysy R, Bielawski K: Novel dinuclear platinum (II) complexes targets NFkappaB signaling pathway to induce apoptosis and inhibit metabolism of MCF-7 breast cancer cells. Folia Histochem Cytobiol. 2009;47(5):S141-6.

Four novel dinuclear platinum (II) complexes of formula [Pt2L4 (berenil) 2] Cl4 (Pt1-Pt4) where L is piperazine (Pt1), 4-picoline (Pt2), 3-picoline (Pt3) or isopropylamine (Pt4) were compared to cisplatin in respect to collagen biosynthesis, beta1- integrin receptor, IGF-I receptor, phosphorylated MAP-kinases (ERK1/ERK2 and p38), phosphorylated Akt kinase expression and appearance of apoptosis in MCF-7 breast cancer cells.
31(0,1,1,1) Details
19619528 Yang J, Yao J, Chen J, Wang XN, Zhu TY, Chen LL, Chu P: Construction of drug screening cell model and application to new compounds inhibiting FITC-fibrinogen binding to CHO cells expressing human alphaIIbbeta3. Eur J Pharmacol. 2009 Sep 15;618(1-3):1-8. Epub 2009 Jul 17.

Our research results indicated that the compounds with phenylsulfonyl (compounds 1 and 2) and benzoyl groups (compounds 4 and 5) at position 4 of piperazine showed higher IC (50) values of inhibiting ADP-induced human platelet aggregation.
MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays showed that compounds 4 and 5 possess potential anti-cancer activities, suggesting a potential role of integrin-guided signal pathway in cancer therapy.
1(0,0,0,1) Details
16309911 Kubota D, Ishikawa M, Yamamoto M, Murakami S, Hachisu M, Katano K, Ajito K: Tricyclic pharmacophore-based molecules as novel integrin alpha (v) beta3 antagonists. Bioorg Med Chem. 2006 Apr 1;14(7):2089-108. Epub 2005 Nov 23.

Although piperazine-containing compounds initially prepared were selective alpha (IIb) beta3 antagonists, replacement of piperazine with piperidine furnished a potent alpha (v) beta3/alpha (IIb) beta3 dual antagonist.
Structure-activity relationship (SAR) studies provided clues for further development of tricyclic pharmacophore-based integrin antagonists.
1(0,0,0,1) Details