Anticancer activities of novel chalcone and bis-chalcone derivatives

Aneta Modzelewska; Catherine Pettit; Geetha Achanta; Nancy E. Davidson; Peng Huang; Saeed R. Khan

doi:10.1016/j.bmc.2006.01.003

Anticancer activities of novel chalcone and bis-chalcone derivatives

Aneta Modzelewska
, Catherine Pettit
, Geetha Achanta
, Nancy E. Davidson
, Peng Huang
, Saeed R. Khan

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

321 Scopus citations

Abstract

A series of novel chalcones and bis-chalcones containing boronic acid moieties has been synthesized and evaluated for antitumor activity against the human breast cancer MDA-MB-231 (estrogen receptor-negative) and MCF7 (estrogen receptor-positive) cell lines and against two normal breast epithelial cell lines, MCF-10A and MCF-12A. These molecules inhibited the growth of the human breast cancer cell lines at low micromolar to nanomolar concentrations, with five of them (1-4, 9) showing preferential inhibition of the human breast cancer cell lines. Furthermore, bis-chalcone 8 exhibited a more potent inhibition of colon cancer cells expressing wild-type p53 than of an isogenic cell line that was p53-null.

Original language	English (US)
Pages (from-to)	3491-3495
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry
Volume	14
Issue number	10
DOIs	https://doi.org/10.1016/j.bmc.2006.01.003
State	Published - May 15 2006
Externally published	Yes

Keywords

Anticancer
Bis-chalcone
Chalcone
Claisen-Schmidt reaction

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmc.2006.01.003

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title = "Anticancer activities of novel chalcone and bis-chalcone derivatives",

abstract = "A series of novel chalcones and bis-chalcones containing boronic acid moieties has been synthesized and evaluated for antitumor activity against the human breast cancer MDA-MB-231 (estrogen receptor-negative) and MCF7 (estrogen receptor-positive) cell lines and against two normal breast epithelial cell lines, MCF-10A and MCF-12A. These molecules inhibited the growth of the human breast cancer cell lines at low micromolar to nanomolar concentrations, with five of them (1-4, 9) showing preferential inhibition of the human breast cancer cell lines. Furthermore, bis-chalcone 8 exhibited a more potent inhibition of colon cancer cells expressing wild-type p53 than of an isogenic cell line that was p53-null.",

keywords = "Anticancer, Bis-chalcone, Chalcone, Claisen-Schmidt reaction",

author = "Aneta Modzelewska and Catherine Pettit and Geetha Achanta and Davidson, \{Nancy E.\} and Peng Huang and Khan, \{Saeed R.\}",

note = "Funding Information: We gratefully acknowledge the financial support of FAMRI, as well as grants CA100428 and CA 88843 from the National Cancer Institute, National Institutes of Health.",

year = "2006",

month = may,

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doi = "10.1016/j.bmc.2006.01.003",

language = "English (US)",

volume = "14",

pages = "3491--3495",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

number = "10",

}

TY - JOUR

T1 - Anticancer activities of novel chalcone and bis-chalcone derivatives

AU - Modzelewska, Aneta

AU - Pettit, Catherine

AU - Achanta, Geetha

AU - Davidson, Nancy E.

AU - Huang, Peng

AU - Khan, Saeed R.

N1 - Funding Information: We gratefully acknowledge the financial support of FAMRI, as well as grants CA100428 and CA 88843 from the National Cancer Institute, National Institutes of Health.

PY - 2006/5/15

Y1 - 2006/5/15

N2 - A series of novel chalcones and bis-chalcones containing boronic acid moieties has been synthesized and evaluated for antitumor activity against the human breast cancer MDA-MB-231 (estrogen receptor-negative) and MCF7 (estrogen receptor-positive) cell lines and against two normal breast epithelial cell lines, MCF-10A and MCF-12A. These molecules inhibited the growth of the human breast cancer cell lines at low micromolar to nanomolar concentrations, with five of them (1-4, 9) showing preferential inhibition of the human breast cancer cell lines. Furthermore, bis-chalcone 8 exhibited a more potent inhibition of colon cancer cells expressing wild-type p53 than of an isogenic cell line that was p53-null.

AB - A series of novel chalcones and bis-chalcones containing boronic acid moieties has been synthesized and evaluated for antitumor activity against the human breast cancer MDA-MB-231 (estrogen receptor-negative) and MCF7 (estrogen receptor-positive) cell lines and against two normal breast epithelial cell lines, MCF-10A and MCF-12A. These molecules inhibited the growth of the human breast cancer cell lines at low micromolar to nanomolar concentrations, with five of them (1-4, 9) showing preferential inhibition of the human breast cancer cell lines. Furthermore, bis-chalcone 8 exhibited a more potent inhibition of colon cancer cells expressing wild-type p53 than of an isogenic cell line that was p53-null.

KW - Anticancer

KW - Bis-chalcone

KW - Chalcone

KW - Claisen-Schmidt reaction

UR - https://www.scopus.com/pages/publications/33645885368

UR - https://www.scopus.com/pages/publications/33645885368#tab=citedBy

U2 - 10.1016/j.bmc.2006.01.003

DO - 10.1016/j.bmc.2006.01.003

M3 - Article

C2 - 16434201

AN - SCOPUS:33645885368

SN - 0968-0896

VL - 14

SP - 3491

EP - 3495

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 10

ER -

Anticancer activities of novel chalcone and bis-chalcone derivatives

Abstract

Keywords

ASJC Scopus subject areas

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