Calcium level controlling activities of novel derivatives of amlodipine, riodipine and cerebrocrast

R. Vilskersts; B. Vigante; Z. Neidere; A. Krauze; I. Domracheva; L. Bekere; I. Shestakova; G. Duburs; M. Dambrova

doi:10.2174/157018012799129909

Calcium level controlling activities of novel derivatives of amlodipine, riodipine and cerebrocrast

R. Vilskersts, B. Vigante, Z. Neidere, A. Krauze, I. Domracheva, L. Bekere, I. Shestakova, G. Duburs, M. Dambrova

Research output: Contribution to journal › Article › peer-review

3 Citations (Scopus)

Abstract

A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC ₅₀=39 μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC ₅₀=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.

Original language	English
Pages (from-to)	322-328
Number of pages	7
Journal	Letters in Drug Design and Discovery
Volume	9
Issue number	3
DOIs	https://doi.org/10.2174/157018012799129909
Publication status	Published - Mar 2012
Externally published	Yes

Keywords*

Amlodipine
Asymmetric 1,4-dihydropyridines
Calcium channel antagonists
Cerebrocrast
Riodipine

Field of Science*

3.1 Basic medicine

Publication Type*

1.1. Scientific article indexed in Web of Science and/or Scopus database

Access to Document

10.2174/157018012799129909

Cite this

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title = "Calcium level controlling activities of novel derivatives of amlodipine, riodipine and cerebrocrast",

abstract = "A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC 50=39 μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC 50=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.",

keywords = "Amlodipine, Asymmetric 1,4-dihydropyridines, Calcium channel antagonists, Cerebrocrast, Riodipine",

author = "R. Vilskersts and B. Vigante and Z. Neidere and A. Krauze and I. Domracheva and L. Bekere and I. Shestakova and G. Duburs and M. Dambrova",

year = "2012",

month = mar,

doi = "10.2174/157018012799129909",

language = "English",

volume = "9",

pages = "322--328",

journal = "Letters in Drug Design and Discovery",

issn = "1570-1808",

publisher = "Bentham Science Publishers",

number = "3",

}

TY - JOUR

T1 - Calcium level controlling activities of novel derivatives of amlodipine, riodipine and cerebrocrast

AU - Vilskersts, R.

AU - Vigante, B.

AU - Neidere, Z.

AU - Krauze, A.

AU - Domracheva, I.

AU - Bekere, L.

AU - Shestakova, I.

AU - Duburs, G.

AU - Dambrova, M.

PY - 2012/3

Y1 - 2012/3

N2 - A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC 50=39 μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC 50=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.

AB - A novel series of asymmetric 4-aryl-1,4-dihydropyridine (1,4-DHP) 3,5-diester derivatives and their symmetric analogues comprised of functional moieties of amlodipine, riodipine and cerebrocrast have been synthesized. The calcium channel blocking activity was evaluated in an isolated rat aortic ring model. The calcium overload preventing activity was tested in SH-SY5Y neuroblastoma cell line by a fluorescence-based calcium assay. Among synthesized and tested compounds, 4a showed the highest calcium overload preventing activity (IC 50=39 μM) and 7e demonstrated the highest calcium channel inhibiting activity (EC 50=0.2 nM). Asymmetric ester 7a exerted both substantial calcium channel blocking and calcium overload preventing activity.

KW - Amlodipine

KW - Asymmetric 1,4-dihydropyridines

KW - Calcium channel antagonists

KW - Cerebrocrast

KW - Riodipine

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U2 - 10.2174/157018012799129909

DO - 10.2174/157018012799129909

M3 - Article

AN - SCOPUS:84858266617

SN - 1570-1808

VL - 9

SP - 322

EP - 328

JO - Letters in Drug Design and Discovery

JF - Letters in Drug Design and Discovery

IS - 3

ER -

Calcium level controlling activities of novel derivatives of amlodipine, riodipine and cerebrocrast

Abstract

Keywords*

Field of Science*

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