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      Synthesis and Cytotoxic Evaluation of Alkoxylated Chalcones

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          Abstract

          A series of chalcones a1– 20 bearing a 4-OMe groups on the A-ring were initially synthesized and their anticancer activities towards HepG2 cells evaluated. Subsequently, a series of chalcones b1– 42 bearing methoxy groups at the 2' and 6'-positions of the B-ring were synthesized and their anticancer activities towards five human cancer cell lines (HepG2, HeLa, MCF-7, A549 and SW1990) and two non-tumoral human cell lines evaluated. The results showed that six compounds ( b6, b8, b11, b16, b18, b22, b23 and b29) displayed promising activities, with compounds b22 and b29 in particular showing higher levels of activity than etoposide against all five cancer cell lines. Compound b29 showed a promising SI value compared with both HMLE and L02 (2.1–6.5 fold in HMLE and > 33 > 103.1 fold in L02, respectively).

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          A review of anti-infective and anti-inflammatory chalcones.

          Z Nowakowska (2007)
          Chalcones, considered as the precursors of flavonoids and isoflavonoids, are abundant in edible plants, and have also been shown to display a diverse array of pharmacological activities. The purpose of this review is to provide an overview of the pharmacological activity of synthetic and naturally occurring chalcones. This review is complementary to earlier reviews and covers more recent reports of antimicrobial activity of chalcones (antibacterial and antifungal), as well as antileishmanial, antimalarial, antiviral and anti-inflammatory activities of these compounds.
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            Evaluation and discovery of novel synthetic chalcone derivatives as anti-inflammatory agents.

            Yong-Xin Pan, Yuepiao Cai, Shulin Yang … (2011)
            Major anti-inflammatory agents, steroids and cyclooxygenase, were proved to have serious side effects. Here, a series of chalcone derivatives were synthesized and screened for anti-inflammatory activities. QSAR study revealed that the presence of electron-withdrawing groups in B-ring and electron-donating groups in A-ring of chalcones was important for inhibition of LPS-induced IL-6 expression. Further, compounds 22, 23, 26, 40, and 47 inhibited TNF-α and IL-6 release in a dose-dependent manner and decreased LPS-induced TNF-α, IL-1β, IL-6, IL-12, and COX-2 mRNA production. Mechanistically, compounds 23 and 26 interfered with JNK/NF-κB signaling and dose-dependently prevented ERK and p38 activation. In addition, 23 and 26 exhibited a significant protection against LPS-induced death and were able to block high glucose-activated cytokine profiles in macrophages. Together, these data show a series of anti-inflammatory chalcones with potential therapeutic effects in inflammatory diseases.
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              Anticancer activities of novel chalcone and bis-chalcone derivatives.

              Alice E. Davidson, Zeyaur Khan, Geetha Achanta … (2006)
              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.
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                Author and article information

                Contributors
                Derek J. McPhee: Role: External Editor
                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules
                Publisher: MDPI
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 28 October 2014
                Publication date Collection: November 2014
                Volume: 19
                Issue: 11
                Pages: 17256-17278
                Affiliations
                Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; E-Mails: baixiaoguang130@ 123456126.com (X.-G.B.); clxu1986@ 123456163.com (C.-L.X.); zhshsh1112@ 123456163.com (S.-S.Z.); hehwei@ 123456163.com (H.W.H.); wyc9999@ 123456126.com (Y.-C.W.)
                Author notes
                [†]

                These authors contributed equally to this work.

                [* ]Author to whom correspondence should be addressed; E-Mail: imbjxwang@ 123456gmail.com ; Tel./Fax: +86-10-6316-5263.
                Article
                Publisher ID: molecules-19-17256
                DOI: 10.3390/molecules191117256
                PMC ID: 6271338
                PubMed ID: 25353380
                SO-VID: f91b26b4-4b60-4846-a339-10f5e7f6d2b7
                Copyright © © 2014 by the authors.
                License:

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/4.0/).

                History
                Date received : 25 July 2014
                Date revision received : 26 September 2014
                Date accepted : 17 October 2014
                Categories
                Subject: Article

                Keywords: alkoxylated chalcones,synthesis,cytotoxicity
                Data availability:
                Keywords: alkoxylated chalcones, synthesis, cytotoxicity

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