Cytotoxic 4′-aminochalcones and related compounds

J. R. Dimmock, A. Jha, G. A. Zello, T. M. Allen, C. L. Santos, J. Balzarini, E. De Clercq, Elias Kurian Manavathu, J. P. Stables

Research output: Contribution to journalArticle

29 Citations (Scopus)

Abstract

A series of 4′-aminochalcones 1 and related maleamic acids 2 and Schiff bases 3 were designed and synthesized as candidate cytotoxic agents. The atomic charges on different atoms of representative compounds were calculated. Evaluation of the enones 1-3 against human Molt 4/C8 and CEM T-lymphocytes as well as murine P388 and L1210 leukemic cells revealed that approximately 40% of the IC50 values generated were less than 10 μM. In some cases cytotoxicity was correlated with the Hammett σ values of the aryl substituents and less frequently with the aryl Hansch π values. Evidence was obtained that in general these compounds displayed selective toxicity for certain malignant cells and were well tolerated in mice. This study has revealed various directions whereby the project may be amplified in the future with a view to finding compounds with increased cytotoxicity to tumour cells.

Original languageEnglish (US)
Pages (from-to)227-232
Number of pages6
JournalPharmazie
Volume58
Issue number4
StatePublished - Apr 1 2003

Fingerprint

Schiff Bases
Cytotoxins
Inhibitory Concentration 50
T-Lymphocytes
Neoplasms
maleamic acid
Direction compound

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Dimmock, J. R., Jha, A., Zello, G. A., Allen, T. M., Santos, C. L., Balzarini, J., ... Stables, J. P. (2003). Cytotoxic 4′-aminochalcones and related compounds. Pharmazie, 58(4), 227-232.

Cytotoxic 4′-aminochalcones and related compounds. / Dimmock, J. R.; Jha, A.; Zello, G. A.; Allen, T. M.; Santos, C. L.; Balzarini, J.; De Clercq, E.; Manavathu, Elias Kurian; Stables, J. P.

In: Pharmazie, Vol. 58, No. 4, 01.04.2003, p. 227-232.

Research output: Contribution to journalArticle

Dimmock, JR, Jha, A, Zello, GA, Allen, TM, Santos, CL, Balzarini, J, De Clercq, E, Manavathu, EK & Stables, JP 2003, 'Cytotoxic 4′-aminochalcones and related compounds', Pharmazie, vol. 58, no. 4, pp. 227-232.
Dimmock JR, Jha A, Zello GA, Allen TM, Santos CL, Balzarini J et al. Cytotoxic 4′-aminochalcones and related compounds. Pharmazie. 2003 Apr 1;58(4):227-232.
Dimmock, J. R. ; Jha, A. ; Zello, G. A. ; Allen, T. M. ; Santos, C. L. ; Balzarini, J. ; De Clercq, E. ; Manavathu, Elias Kurian ; Stables, J. P. / Cytotoxic 4′-aminochalcones and related compounds. In: Pharmazie. 2003 ; Vol. 58, No. 4. pp. 227-232.
@article{40d9a4b54f684f58b28f03e2ef42f4cc,
title = "Cytotoxic 4′-aminochalcones and related compounds",
abstract = "A series of 4′-aminochalcones 1 and related maleamic acids 2 and Schiff bases 3 were designed and synthesized as candidate cytotoxic agents. The atomic charges on different atoms of representative compounds were calculated. Evaluation of the enones 1-3 against human Molt 4/C8 and CEM T-lymphocytes as well as murine P388 and L1210 leukemic cells revealed that approximately 40{\%} of the IC50 values generated were less than 10 μM. In some cases cytotoxicity was correlated with the Hammett σ values of the aryl substituents and less frequently with the aryl Hansch π values. Evidence was obtained that in general these compounds displayed selective toxicity for certain malignant cells and were well tolerated in mice. This study has revealed various directions whereby the project may be amplified in the future with a view to finding compounds with increased cytotoxicity to tumour cells.",
author = "Dimmock, {J. R.} and A. Jha and Zello, {G. A.} and Allen, {T. M.} and Santos, {C. L.} and J. Balzarini and {De Clercq}, E. and Manavathu, {Elias Kurian} and Stables, {J. P.}",
year = "2003",
month = "4",
day = "1",
language = "English (US)",
volume = "58",
pages = "227--232",
journal = "Die Pharmazie",
issn = "0031-7144",
publisher = "Govi-Verlag Pharmazeutischer Verlag GmbH",
number = "4",

}

TY - JOUR

T1 - Cytotoxic 4′-aminochalcones and related compounds

AU - Dimmock, J. R.

AU - Jha, A.

AU - Zello, G. A.

AU - Allen, T. M.

AU - Santos, C. L.

AU - Balzarini, J.

AU - De Clercq, E.

AU - Manavathu, Elias Kurian

AU - Stables, J. P.

PY - 2003/4/1

Y1 - 2003/4/1

N2 - A series of 4′-aminochalcones 1 and related maleamic acids 2 and Schiff bases 3 were designed and synthesized as candidate cytotoxic agents. The atomic charges on different atoms of representative compounds were calculated. Evaluation of the enones 1-3 against human Molt 4/C8 and CEM T-lymphocytes as well as murine P388 and L1210 leukemic cells revealed that approximately 40% of the IC50 values generated were less than 10 μM. In some cases cytotoxicity was correlated with the Hammett σ values of the aryl substituents and less frequently with the aryl Hansch π values. Evidence was obtained that in general these compounds displayed selective toxicity for certain malignant cells and were well tolerated in mice. This study has revealed various directions whereby the project may be amplified in the future with a view to finding compounds with increased cytotoxicity to tumour cells.

AB - A series of 4′-aminochalcones 1 and related maleamic acids 2 and Schiff bases 3 were designed and synthesized as candidate cytotoxic agents. The atomic charges on different atoms of representative compounds were calculated. Evaluation of the enones 1-3 against human Molt 4/C8 and CEM T-lymphocytes as well as murine P388 and L1210 leukemic cells revealed that approximately 40% of the IC50 values generated were less than 10 μM. In some cases cytotoxicity was correlated with the Hammett σ values of the aryl substituents and less frequently with the aryl Hansch π values. Evidence was obtained that in general these compounds displayed selective toxicity for certain malignant cells and were well tolerated in mice. This study has revealed various directions whereby the project may be amplified in the future with a view to finding compounds with increased cytotoxicity to tumour cells.

UR - http://www.scopus.com/inward/record.url?scp=0037399361&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0037399361&partnerID=8YFLogxK

M3 - Article

C2 - 12749401

AN - SCOPUS:0037399361

VL - 58

SP - 227

EP - 232

JO - Die Pharmazie

JF - Die Pharmazie

SN - 0031-7144

IS - 4

ER -