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

Deadline for manuscript submissions: closed (30 September 2021) | Viewed by 35693

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Prof. Dr. Qiao-Hong Chen

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Department of Chemistry and Biochemistry, California State University, Fresno 2555 E. San Ramon Ave. M/S SB70, Fresno, CA 93740, USA
Interests: anticancer agents; medicinal chemistry; natural products; bioorganic chemistry; organic synthesis; drug design and synthesis; prostate cancer; lead compound optimization; biological evaluation
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Dear Colleagues,

The cancer-related mortality rate still remains high due to the various limitations of currently available therapies. 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 to the rational design of new anticancer agents. Numerous well-established synthetic methods and biological screening assays pave the avenue for the discovery and development of new anticancer agents. The second edition of this Special Issue of Molecules continues to be devoted to all aspects of recent exploitation for new anticancer agents. Both original research and review articles, focusing on rational design, synthesis, and/or biological evaluation of various agents (including small molecules, natural products, endogenous molecules, antibodies and vaccines) as potential cancer therapeutics, are welcome to be submitted for publication in this Special Issue.

Dr. Qiao-Hong Chen
Guest Editor

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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

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Related Special Issues

Anticancer Agents: Design, Synthesis and Evaluation in Molecules (32 articles)
Anticancer Agents: Design, Synthesis and Evaluation III in Molecules (10 articles)

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Research

19 pages, 2734 KiB

Open AccessArticle

Design, Synthesis and Tumour-Selective Toxicity of Novel 1-[3-{3,5-Bis(benzylidene)-4-oxo-1-piperidino}-3-oxopropyl]-4-piperidone Oximes and Related Quaternary Ammonium Salts

by Praveen K. Roayapalley, Jonathan R. Dimmock, Lisett Contreras, Karol S. Balderrama, Renato J. Aguilera, Hiroshi Sakagami, Shigeru Amano, Rajendra K. Sharma and Umashankar Das

Molecules 2021, 26(23), 7132; https://doi.org/10.3390/molecules26237132 - 25 Nov 2021

Cited by 4 | Viewed by 2036

Abstract

A novel series of 1-[3-{3,5-bis(benzylidene)-4-oxo-1-piperidino}-3-oxopropyl]-4-piperidone oximes 3a–h and related quaternary ammonium salts 4a–h were prepared as candidate antineoplastic agents. Evaluation against neoplastic Ca9-22, HSC-2 and HSC-4 cells revealed the compounds in series 3 and 4 to be potent cytotoxins with submicromolar CC₅₀ values in virtually all cases. In contrast, the compounds were less cytocidal towards HGF, HPLF and HPC non-malignant cells revealing their tumour-selective toxicity. Quantitative structure–activity relationships revealed that, in general, both cytotoxic potency and selectivity index figures increased as the magnitude of the Hammett sigma values rose. In addition, 3a–h are cytotoxic towards a number of leukemic and colon cancer cells. 4b,c lowered the mitochondrial membrane potential in CEM cells, and 4d induced transient G2/M accumulation in Ca9-22 cells. Five compounds, namely 3c,d and 4c–e, were identified as lead molecules that have drug-like properties. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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16 pages, 3791 KiB

Open AccessArticle

Homocystamide Conjugates of Human Serum Albumin as a Platform to Prepare Bimodal Multidrug Delivery Systems for Boron Neutron Capture Therapy

by Tatyana Popova, Maya A. Dymova, Ludmila S. Koroleva, Olga D. Zakharova, Vladimir A. Lisitskiy, Valeria I. Raskolupova, Tatiana Sycheva, Sergei Taskaev, Vladimir N. Silnikov and Tatyana S. Godovikova

Molecules 2021, 26(21), 6537; https://doi.org/10.3390/molecules26216537 - 29 Oct 2021

Cited by 6 | Viewed by 2893

Abstract

Boron neutron capture therapy is a unique form of adjuvant cancer therapy for various malignancies including malignant gliomas. The conjugation of boron compounds and human serum albumin (HSA)—a carrier protein with a long plasma half-life—is expected to extend systemic circulation of the boron compounds and increase their accumulation in human glioma cells. We report on the synthesis of fluorophore-labeled homocystamide conjugates of human serum albumin and their use in thiol-‘click’ chemistry to prepare novel multimodal boronated albumin-based theranostic agents, which could be accumulated in tumor cells. The novelty of this work involves the development of the synthesis methodology of albumin conjugates for the imaging-guided boron neutron capture therapy combination. Herein, we suggest using thenoyltrifluoroacetone as a part of an anticancer theranostic construct: approximately 5.4 molecules of thenoyltrifluoroacetone were bound to each albumin. Along with its beneficial properties as a chemotherapeutic agent, thenoyltrifluoroacetone is a promising magnetic resonance imaging agent. The conjugation of bimodal HSA with undecahydro-closo-dodecaborate only slightly reduced human glioma cell line viability in the absence of irradiation (~30 μM of boronated albumin) but allowed for neutron capture and decreased tumor cell survival under epithermal neutron flux. The simultaneous presence of undecahydro-closo-dodecaborate and labeled amino acid residues (fluorophore dye and fluorine atoms) in the obtained HSA conjugate makes it a promising candidate for the combination imaging-guided boron neutron capture therapy. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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16 pages, 1807 KiB

Open AccessArticle

3-O-Carbamoyl-5,7,20-O-trimethylsilybins: Synthesis and Preliminary Antiproliferative Evaluation

by Sitong Wu, Guanglin Chen, Qiang Zhang, Guangdi Wang and Qiao-Hong Chen

Molecules 2021, 26(21), 6421; https://doi.org/10.3390/molecules26216421 - 24 Oct 2021

Cited by 1 | Viewed by 2356

Abstract

To search for novel androgen receptor (AR) modulators for the potential treatment of castration-resistant prostate cancer (CRPC), naturally occurring silibinin was sought after as a lead compound because it possesses a moderate potency towards AR-positive prostate cancer cells and its chemical scaffold is dissimilar to all currently marketed AR antagonists. On the basis of the structure–activity relationships that we have explored, this study aims to incorporate carbamoyl groups to the alcoholic hydroxyl groups of silibinin to improve its capability in selectively suppressing AR-positive prostate cancer cell proliferation together with water solubility. To this end, a feasible approach was developed to regioselectively introduce a carbamoyl group to the secondary alcoholic hydroxyl group at C-3 without causing the undesired oxidation at C2–C3, providing an avenue for achieving 3-O-carbamoyl-5,7,20-O-trimethylsilybins. The application of the synthetic method can be extended to the synthesis of 3-O-carbamoyl-3′,4′,5,7-O-tetramethyltaxifolins. The antiproliferative potency of 5,7,20-O-trimethylsilybin and its nine 3-carbamoyl derivatives were assessed in an AR-positive LNCaP prostate cancer cell line and two AR-null prostate cancer cell lines (PC-3 and DU145). Our preliminary bioassay data imply that 5,7,20-O-trimethylsilybin and four 3-O-carbamoyl-5,7,20-O-trimethylsilybins emerge as very promising lead compounds due to the fact that they can selectively suppress AR-positive LNCaP cell proliferation. The IC₅₀ values of these five 5,7,20-O-trimethylsilybins against the LNCaP cells fall into the range of 0.11–0.83 µM, which exhibit up to 660 times greater in vitro antiproliferative potency than silibinin. Our findings suggest that carbamoylated 5,7,20-O-trimethylsilybins could serve as a natural product-based scaffold for new antiandrogens for lethal castration-resistant prostate cancer. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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10 pages, 2487 KiB

Open AccessArticle

Synthesis, Anti-Proliferative Evaluation and Mechanism of 4-Trifluoro Methoxy Proguanil Derivatives with Various Carbon Chain Length

by Simeng Xu, Yufang Cao, Yu Luo, Di Xiao, Wei Wang, Zhiren Wang and Xiaoping Yang

Molecules 2021, 26(19), 5775; https://doi.org/10.3390/molecules26195775 - 24 Sep 2021

Cited by 3 | Viewed by 2189

Abstract

Among the known biguanide drugs, proguanil has the best antiproliferative activity. In contrast, newly synthesized biguanide derivatives containing fluorine atoms have excellent biological activity, among which trifluoromethoxy compounds show the strongest ability. Preliminary work in our laboratory exhibited that n-heptyl containing proguanil derivatives on one alkyl chain side have better biological activity than those with a shorter carbon chain. However, the relationship between the length of the carbon chain and the activity of the compounds is unknown. In this study, we synthesized 10 new trifluoromethoxy-containing proguanil derivatives with various carbon chain lengths. The phenyl side is fixed as the trifluoromethoxy group with change of carbon chain length in alkyl chain side. It was found that the anti-cancer abilities of 5C–8C with n-pentyl to n-octyl groups was significantly better than that of proguanil in the five human cancer cell lines. The colony formation assay demonstrated that 6C–8C at 0.5 to 1.0 μM significantly inhibited the colony formation of human cancer cell lines, much stronger than that of proguanil. Pharmacologically, 8C activates AMPK, leading to inactivation of the mTOR/p70S6K/4EBP1 pathway. Thus, these novel compounds have a great potential for developing new anti-cancer candidates. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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11 pages, 2714 KiB

Open AccessArticle

Hispolon Induces Apoptosis, Suppresses Migration and Invasion of Glioblastoma Cells and Inhibits GBM Xenograft Tumor Growth In Vivo

by Kuan-Fu Liao, Tsung-Lang Chiu, Shu-Fang Chang, Mei-Jen Wang and Sheng-Chun Chiu

Molecules 2021, 26(15), 4497; https://doi.org/10.3390/molecules26154497 - 26 Jul 2021

Cited by 12 | Viewed by 2553

Abstract

Hispolon, a polyphenol compound isolated from Phellinus linteus, has been reported to exhibit antioxidant, antiproliferative, and antitumor activities. This study aimed to explore the antitumor effects of hispolon on glioblastoma multiforme (GBM) cells in vitro and in vivo. The results revealed that hispolon significantly inhibited GBM cell proliferation and induced apoptosis through caspase-9 and caspase-3 activation and PARP cleavage. Hispolon also induced cell cycle G2/M phase arrest in GBM cells, as supported by flow cytometry analysis and confirmed by a decrease in cyclin B1, cdc2, and cdc25c protein expressions in a dose- and time-dependent manner. Furthermore, hispolon suppressed the migration and invasion of GBM cells by modulating epithelial–mesenchymal transition (EMT) markers via wound healing, transwell assays, and real-time PCR. Moreover, hispolon significantly reduced tumor growth in DBTRG xenograft mice and activated caspase-3 in hispolon-treated tumors. Thus, our findings revealed that hispolon is a potential candidate for the treatment of GBM. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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14 pages, 4255 KiB

Open AccessArticle

Design, Synthesis and Anticancer Activity of a New Series of N-aryl-N′-[4-(pyridin-2-ylmethoxy)benzyl]urea Derivatives

by Shicheng Hou, Shishao Liang, Chao Zhang, Yingmei Han, Jianhui Liang, Hongyu Hu, Xingeng Zhang, Chun Hu, Xiaoping Liu and Hong Zhang

Molecules 2021, 26(12), 3496; https://doi.org/10.3390/molecules26123496 - 8 Jun 2021

Cited by 3 | Viewed by 2465

Abstract

The development of cancer treatments requires continuous exploration and improvement, in which the discovery of new drugs for the treatment of cancer is still an important pathway. In this study, based on the molecular hybridization strategy, a new structural framework with an N-aryl-N’-arylmethylurea scaffold was designed, and 16 new target compounds were synthesized and evaluated for their antiproliferative activities against four different cancer cell lines A549, MCF7, HCT116, PC3, and human liver normal cell line HL7702. The results have shown seven compounds with 1-methylpiperidin-4-yl groups having excellent activities against all four cancer cell lines, and they exhibited scarcely any activities against HL7702. Among them, compound 9b and 9d showed greatly excellent activity against the four kinds of cells, and the IC₅₀ for MCF7 and PC3 cell lines were even less than 3 μM. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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19 pages, 3293 KiB

Open AccessArticle

New Estrone Oxime Derivatives: Synthesis, Cytotoxic Evaluation and Docking Studies

by Catarina Canário, Mariana Matias, Vanessa Brito, Adriana O. Santos, Amílcar Falcão, Samuel Silvestre and Gilberto Alves

Molecules 2021, 26(9), 2687; https://doi.org/10.3390/molecules26092687 - 4 May 2021

Cited by 9 | Viewed by 3109

Abstract

The interest in the introduction of the oxime group in molecules aiming to improve their biological effects is increasing. This work aimed to develop new steroidal oximes of the estrane series with potential antitumor interest. For this, several oximes were synthesized by reaction of hydroxylamine with the 17-ketone of estrone derivatives. Then, their cytotoxicity was evaluated in six cell lines. An estrogenicity assay, a cell cycle distribution analysis and a fluorescence microscopy study with Hoechst 3358 staining were performed with the most promising compound. In addition, molecular docking studies against estrogen receptor α, steroid sulfatase, 17β-hydroxysteroid dehydrogenase type 1 and β-tubulin were also accomplished. The 2-nitroestrone oxime showed higher cytotoxicity than the parent compound on MCF-7 cancer cells. Furthermore, the oximes bearing halogen groups in A-ring evidenced selectivity for HepaRG cells. Remarkably, the Δ^9,11-estrone oxime was the most cytotoxic and arrested LNCaP cells in the G₂/M phase. Fluorescence microscopy studies showed the presence of condensed DNA typical of prophase and condensed and fragmented nuclei characteristic of apoptosis. However, this oxime promoted the proliferation of T47-D cells. Interestingly, molecular docking studies estimated a strong interaction between Δ^9,11-estrone oxime and estrogen receptor α and β-tubulin, which may account for the described effects. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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26 pages, 9265 KiB

Open AccessArticle

Discovery of New Coumarin-Based Lead with Potential Anticancer, CDK4 Inhibition and Selective Radiotheranostic Effect: Synthesis, 2D & 3D QSAR, Molecular Dynamics, In Vitro Cytotoxicity, Radioiodination, and Biodistribution Studies

by Mona O. Sarhan, Somaia S. Abd El-Karim, Manal M. Anwar, Raghda H. Gouda, Wafaa A. Zaghary and Mohammed A. Khedr

Molecules 2021, 26(8), 2273; https://doi.org/10.3390/molecules26082273 - 14 Apr 2021

Cited by 18 | Viewed by 3241

Abstract

Novel 6-bromo-coumarin-ethylidene-hydrazonyl-thiazolyl and 6-bromo-coumarin-thiazolyl-based derivatives were synthesized. A quantitative structure activity relationship (QSAR) model with high predictive power r² = 0.92, and RMSE = 0.44 predicted five compounds; 2b, 3b, 5a, 9a and 9i to have potential anticancer activities. Compound 2b achieved the best ΔG of –15.34 kcal/mol with an affinity of 40.05 pki. In a molecular dynamic study 2b showed an equilibrium at 0.8 Å after 3.5 ns, while flavopiridol did so at 0.5 Å after the same time (3.5 ns). 2b showed an IC₅₀ of 0.0136 µM, 0.015 µM, and 0.054 µM against MCF-7, A-549, and CHO-K1 cell lines, respectively. The CDK4 enzyme assay revealed the significant CDK4 inhibitory activity of compound 2b with IC₅₀ of 0.036 µM. The selectivity of the newly discovered lead compound 2b toward localization in tumor cells was confirmed by a radioiodination biological assay that was done via electrophilic substitution reaction utilizing the oxidative effect of chloramine-t. ¹³¹I-2b showed good in vitro stability up to 4 h. In solid tumor bearing mice, the values of tumor uptake reached a height of 5.97 ± 0.82%ID/g at 60 min p.i. ¹³¹I-2b can be considered as a selective radiotheranostic agent for solid tumors with promising anticancer activity. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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13 pages, 2151 KiB

Open AccessArticle

Synthesis and Antiproliferatory Activities Evaluation of Multi-Substituted Isatin Derivatives

by Ying Ding, Lianbo Zhao, Ying Fu, Lei Hao, Yupeng Fu, Yuan Yuan, Peng Yu and Yuou Teng

Molecules 2021, 26(1), 176; https://doi.org/10.3390/molecules26010176 - 31 Dec 2020

Cited by 8 | Viewed by 3436

Abstract

A series of multi-substituted isatin derivatives were synthesized using the powerful Sandmeyer reaction. The structures of these derivatives were confirmed by ¹H-NMR, ¹³C-NMR, and HR-MS. Inhibition of proliferation activities of these derivatives against human leukemia cells (K562), human hepatocellular carcinoma cells (HepG2) and human colon carcinoma cells (HT-29) were evaluated in vitro using the MTT assay. Among the series, compound 4l exhibited strong antiproliferatory activities against K562, HepG2 and HT-29 cells with IC₅₀ values of 1.75, 3.20, and 4.17 μM, respectively. The morphological, growth inhibitory and apoptosic effects of compound 4l in K562 cells, wound healing effect in HepG2 cells, and tube formating effect in matrix gel of HUVEC cells were evaluated consequently. All results indicated that compound 4l could be used as a potential antitumor agent in further investigations. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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11 pages, 405 KiB

Open AccessCommunication

Discovery of Novel Symmetrical 1,4-Dihydropyridines as Inhibitors of Multidrug-Resistant Protein (MRP4) Efflux Pump for Anticancer Therapy

by Henry Döring, David Kreutzer, Christoph Ritter and Andreas Hilgeroth

Molecules 2021, 26(1), 18; https://doi.org/10.3390/molecules26010018 - 22 Dec 2020

Cited by 10 | Viewed by 5034 | Correction

Abstract

Despite the development of targeted therapies in cancer, the problem of multidrug resistance (MDR) is still unsolved. Most patients with metastatic cancer die from MDR. Transmembrane efflux pumps as the main cause of MDR have been addressed by developed inhibitors, but early inhibitors of the most prominent and longest known efflux pump P-glycoprotein (P-gp) were disappointing. Those inhibitors have been used without knowledge about the expression of P-gp by the treated tumor. Therefore the use of inhibitors of transmembrane efflux pumps in clinical settings is reconsidered as a promising strategy in the case of the respective efflux pump expression. We discovered novel symmetric inhibitors of the symmetric efflux pump MRP4 encoded by the ABCC4 gene. MRP4 is involved in many kinds of cancer with resistance to anticancer drugs. All compounds showed better activities than the best known MRP4 inhibitor MK571 in an MRP4-overexpressing cell line assay, and the activities could be related to the various substitution patterns of aromatic residues within the symmetric molecular framework. One of the best compounds was demonstrated to overcome the MRP4-mediated resistance in the cell line model to restore the anticancer drug sensitivity as a proof of concept. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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20 pages, 11268 KiB

Open AccessArticle

ST09, A Novel Curcumin Derivative, Blocks Cell Migration by Inhibiting Matrix Metalloproteases in Breast Cancer Cells and Inhibits Tumor Progression in EAC Mouse Tumor Models

by Snehal Nirgude, Raghunandan Mahadeva, Jinsha Koroth, Sujeet Kumar, Kothanahally S. Sharath Kumar, Vidya Gopalakrishnan, Subhas S Karki and Bibha Choudhary

Molecules 2020, 25(19), 4499; https://doi.org/10.3390/molecules25194499 - 30 Sep 2020

Cited by 32 | Viewed by 5197

Abstract

Purpose: Curcumin is known for its anticancer and migrastatic activity in various cancers, including breast cancer. Newer curcumin derivatives are being explored to overcome limitations of curcumin like low bioavailability, stability, and side effects due to its higher dose. In this study, the synthesis of ST09, a novel curcumin derivative, and its antiproliferative, cytotoxic, and migrastatic properties have been explored both in vitro and in vivo. Methods: After ST09 synthesis, anticancer activity was studied by performing standard cytotoxicity assays namely, lactate dehydrogenase (LDH) release assay, 3-(4, 5-dimethylthiazol-2-yl)-2–5-diphenyletrazolium bromide (MTT), and trypan blue exclusion assay. Annexin-FITC, cell cycle analysis using flow cytometry, and Western blotting were performed to elucidate cell death mechanisms. The effect on the inhibition of cell migration was studied by transwell migration assay. An EAC (Ehrlich Ascites carcinoma) induced mouse tumor model was used to study the effect of ST09 on tumor regression. Drug toxicity was measured using aspartate aminotransferase (AST), alanine aminotransferase (ALT), blood urea nitrogen (BUN), and flow-cytometry based lymphocyte count. Histological analysis was performed for assessment of any tissue injury post ST09 treatment. Results: ST09 shows an approximate 100-fold higher potency than curcumin, its parent compound, on breast tumor cell lines MCF-7 and MDA-MB231. ST09 arrests the cell cycle in a cell type-specific manner and induces an intrinsic apoptotic pathway both in vitro and in vivo. ST09 inhibits migration by downregulating matrix metalloprotease 1,2 (MMP1,2) and Vimentin. In vivo, ST09 administration led to decreased tumor volume in a mouse allograft model by boosting immunity with no significant drug toxicity. Conclusion: ST09 exhibits antiproliferative and cytotoxic activity at nanomolar concentrations. It induces cell death by activation of the intrinsic pathway of apoptosis both in vitro and in vivo. It also inhibits migration and invasion. This study provides evidence that ST09 can potentially be developed as a novel antitumor drug candidate for highly metastatic and aggressive breast cancer. Full article

(This article belongs to the Special Issue Anticancer Agents: Design, Synthesis and Evaluation II)

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