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Special Issue "Anticancer Agents: Design, Synthesis and Evaluation"

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 March 2020

Special Issue Editor

Guest Editor
Assoc. Prof. Dr. Qiao-Hong Chen

Department of Chemistry, California State University, Fresno 2555 E. San Ramon Ave. M/S SB70 Fresno, CA 93740, USA
Website | E-Mail
Phone: +559-278-2394
Interests: anticancer agents; medicinal chemistry; natural products; bioorganic chemistry; organic synthesis; drug design and synthesis; prostate cancer; lead compound optimization; biological evaluation

Special Issue Information

Dear Colleagues,

The currently available cancer therapies still have various limitations, such as multi-drug resistance, undesired off-target effects, and unpredictable efficacies. The cancer-related mortality rate still remains high. The development of novel anticancer agents thus continues to be imperative to combat various deadly cancers. The emerging molecular targets and signal pathways enable the development of novel strategies for the rational design of new anticancer agents. Numerous well-established synthetic methods and biological screening assays have paved the way for the discovery and development of new anticancer agents. This Special Issue of Molecules is devoted to all aspects of recent studies searching for new anticancer agents. Both original research and review articles focusing on the rational design, synthesis, and/or biological evaluation of various agents (including small molecules, natural products, intrinsic molecules, antibodies and vaccines) as potential cancer therapeutics are welcome to be submitted for publication in this Special Issue.

Assoc. Prof. Dr. Qiao-Hong Chen
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • cancer drug discovery
  • cancer drug development
  • medicinal synthesis
  • cancer therapy
  • chemotherapeutics
  • anticancer activity
  • rational drug design
  • Structure-activity relationship
  • cancer therapeutics
  • anticancer agent
  • antitumor agent
  • biological evaluation
  • cancer bioassay
  • cancer screening assay
  • natural product
  • small molecule enzyme inhibitor
  • receptor antagonist
  • lead optimization
  • structure modification
  • structure manipulation
  • anti-proliferative activity
  • cytotoxicity
  • cell apoptosis
  • cancer cell models
  • anti-tumor efficacy

Published Papers (3 papers)

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Research

Open AccessArticle
Design and Synthesis of Flavonoidal Ethers and Their Anti-Cancer Activity In Vitro
Molecules 2019, 24(9), 1749; https://doi.org/10.3390/molecules24091749
Received: 30 March 2019 / Revised: 2 May 2019 / Accepted: 3 May 2019 / Published: 6 May 2019
PDF Full-text (869 KB) | HTML Full-text | XML Full-text
Abstract
Flavonoids are well-characterized polyphenolic compounds with pharmacological and therapeutic activities. However, most flavonoids have not been developed into clinical drugs, due to poor bioavailability. Herein, we report a strategy to increase the drugability of flavonoids by constructing C(sp2)-O bonds and stereo- [...] Read more.
Flavonoids are well-characterized polyphenolic compounds with pharmacological and therapeutic activities. However, most flavonoids have not been developed into clinical drugs, due to poor bioavailability. Herein, we report a strategy to increase the drugability of flavonoids by constructing C(sp2)-O bonds and stereo- as well as regioselective alkenylation of hydroxyl groups of flavonoids with ethyl-2,3-butadienoate allenes. Twenty-three modified flavonoid derivatives were designed, synthesized, and evaluated for their anti-cancer activities. The results showed that compounds 4b, 4c, 4e, 5e, and 6b exhibited better in vitro inhibitory activity against several cancer cell lines than their precursors. Preliminary structure–activity relationship studies indicated that, in most of the cancer cell lines evaluated, the substitution on position 7 was essential for increasing cytotoxicity. The results of this study might facilitate the preparation or late-stage modification of complex flavonoids as anti-cancer drug candidates. Full article
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation)
Figures

Figure 1

Open AccessArticle
Design, Synthesis, and Mechanism of Dihydroartemisinin–Coumarin Hybrids as Potential Anti-Neuroinflammatory Agents
Molecules 2019, 24(9), 1672; https://doi.org/10.3390/molecules24091672
Received: 6 April 2019 / Revised: 23 April 2019 / Accepted: 24 April 2019 / Published: 28 April 2019
Cited by 1 | PDF Full-text (3786 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Cancer patients frequently suffer from cancer-related fatigue (CRF), which is a complex syndrome associated with weakness and depressed mood. Neuroinflammation is one of the major inducers of CRF. The aim of this study is to find a potential agent not only on the [...] Read more.
Cancer patients frequently suffer from cancer-related fatigue (CRF), which is a complex syndrome associated with weakness and depressed mood. Neuroinflammation is one of the major inducers of CRF. The aim of this study is to find a potential agent not only on the treatment of cancer, but also for reducing CRF level of cancer patients. In this study, total-thirty new Dihydroartemisinin–Coumarin hybrids (DCH) were designed and synthesized. The in vitro cytotoxicity against cancer cell lines (HT-29, MDA-MB-231, HCT-116, and A549) was evaluated. Simultaneously, we also tested the anti-neuroinflammatory activity of DCH. DCH could inhibit the activated microglia N9 release of NO, TNF-α, and IL-6. The docking analysis was shown that MD-2, the coreceptor of TLR4, might be one of the targets of DCH. Full article
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation)
Figures

Figure 1

Open AccessArticle
Synthesis of New Derivatives of Benzofuran as Potential Anticancer Agents
Molecules 2019, 24(8), 1529; https://doi.org/10.3390/molecules24081529
Received: 28 March 2019 / Revised: 15 April 2019 / Accepted: 16 April 2019 / Published: 18 April 2019
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Abstract
The results of our previous research indicated that some derivatives of benzofurans, particularly halogeno-derivatives, are selectively toxic towards human leukemia cells. Continuing our work with this group of compounds we here report new data on the synthesis as well as regarding the physico-chemical [...] Read more.
The results of our previous research indicated that some derivatives of benzofurans, particularly halogeno-derivatives, are selectively toxic towards human leukemia cells. Continuing our work with this group of compounds we here report new data on the synthesis as well as regarding the physico-chemical and biological characterization of fourteen new derivatives of benzofurans, including six brominated compounds. The structures of all new compounds were established by spectroscopic methods (1H- and, 13C-NMR, ESI MS), and elemental analyses. Their cytotoxicity was evaluated against K562 (leukemia), MOLT-4 (leukemia), HeLa (cervix carcinoma), and normal cells (HUVEC). Five compounds (1c, 1e, 2d, 3a, 3d) showed significant cytotoxic activity against all tested cell lines and selectivity for cancer cell lines. The SAR analysis (structure-activity relationship analysis) indicated that the presence of bromine introduced to a methyl or acetyl group that was attached to the benzofuran system increased their cytotoxicity both in normal and cancer cells. Full article
(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation)
Figures

Graphical abstract

Planned Papers

The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.

Title: Enzalutamide and Its Analogs as Therapeutics for Castration-Resistant Prostate Cancer
Article Type: Review
Authors: Pravien Rajaram, Qiao-Hong Chen *
Abstract: Enzalutamide is a synthetic second-generation androgen receptor (AR) antagonist with a strong binding affinity to AR. Most importantly, enzalutamide can significantly prolong overall survival time for patients with lethal castration-resistant prostate cancer (CRPC). Enzalutamide has thus been approved by the US Food and Drug Administration for the treatment of both metastatic (in 2012) and non-metastatic (in 2018) CRPC. This review will cover the rational design and development of enzalutamide, and will then describe its synthesis, medicinal chemistry, mechanisms of action, and pharmacokinetic profiles. The interaction of enzalutamide with other chemotherapeutics and the mechanisms of enzalutamide resistance will also be summarized.

Title: Itaconic-quinoline hybrids as potential anticancer agents
Article Type: Article
Author: Branka Zorc

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