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Synthesis and Biological Evaluation of Novel Drugs as Anticancer Agents
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Synthesis and Biological Evaluation of Novel Drugs as Anticancer Agents

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

Deadline for manuscript submissions: closed (31 October 2022) | Viewed by 15763

Special Issue Editors

Dr. Wen-Wei Qiu

E-Mail Website
Guest Editor
School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China
Interests: organic synthesis; medicinal chemistry; drug synthesis; biological evaluation; anticancer agents
Special Issues, Collections and Topics in MDPI journals
Dr. Wenlong Wang

E-Mail Website
Guest Editor
School of Pharmaceutical Sciences, Jiangnan University, Wuxi 214122, China
Interests: drug discovery; anti-HBV drug; drug synthesis; protein tyrosine phosphatase; Inhibitor design; biological evaluation

Special Issue Information

Dear Colleagues,

Cancer is one of the most life-threating diseases and is considered a major worldwide health problem. It causes about 550,000 deaths each year and is currently the second leading cause of death in the world. Cancer continues to pose great challenges to medical science. Cancer is extremely complex, affecting nearly every tissue lineage in body and arising from normal cells as a consequence of diverse mutations affecting many genes. The development of novel molecularly targeted cancer therapeutics remains slow and expensive with many failures. Although numerous drugs have been used for cancer treatment, and because most drugs are not able to discriminate between cancerous and normal cell types, meaning that they can cause serious side effects that are often cumulative and dose limiting, continuous efforts should be made toward the design and synthesis of more effective and more selective novel anticancer drug candidates with promising activity and minimal side effects.

Dr. Wen-Wei Qiu
Dr. Wenlong Wang
Guest Editors

Manuscript Submission Information

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Keywords

  • anticancer
  • biological activity
  • synthesis
  • agents
  • selectivity
  • side effects

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Published Papers (5 papers)

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Research

19 pages, 2660 KiB  
Article
Design of Conjugates Based on Sesquiterpene Lactones with Polyalkoxybenzenes by “Click” Chemistry to Create Potential Anticancer Agents
by Margarita E. Neganova, Ekaterina V. Smirnova, Elena V. Sharova, Oleg I. Artyushin, Yulia R. Aleksandrova, Ekaterina Yu. Yandulova, Natalia S. Nikolaeva and Valery K. Brel
Molecules 2022, 27(23), 8411; https://doi.org/10.3390/molecules27238411 - 1 Dec 2022
Cited by 9 | Viewed by 1954
Abstract
Using the methodology of “click” chemistry, a singular method has been developed for the synthesis of unique conjugates based on sesquiterpene lactones: dehydrocostuslactone and alantolactone with polyalkoxybenzenes. To expand the structural range of the resulting conjugates, the length of the 1,2,3-triazole spacer was [...] Read more.
Using the methodology of “click” chemistry, a singular method has been developed for the synthesis of unique conjugates based on sesquiterpene lactones: dehydrocostuslactone and alantolactone with polyalkoxybenzenes. To expand the structural range of the resulting conjugates, the length of the 1,2,3-triazole spacer was varied. For all synthesized compounds, the cytotoxic profile was determined on the cell lines of tumor origin (SH-SY5Y, HeLa, Hep-2, A549) and normal Hek 293 cells. It was found that the compounds based on alantolactone 7a–d with a long spacer and substances containing dehydrocostuslactone 10a–d with a short spacer have the greatest toxic effect. The decrease in cell survival under the action of these conjugates may be due to their ability to cause dissipation of the transmembrane potential of mitochondria and inhibit the process of glycolysis, leading to cell death. The obtained results confirm the assumption that the development of conjugates based on sesquiterpene lactones and polyalkoxybenzenes can be considered as a promising strategy for the search for potential antitumor agents. Full article
(This article belongs to the Special Issue Synthesis and Biological Evaluation of Novel Drugs as Anticancer Agents)
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17 pages, 3550 KiB  
Article
Design, Cytotoxicity and Antiproliferative Activity of 4-Amino-5-methyl-thieno[2,3-d]pyrimidine-6-carboxylates against MFC-7 and MDA-MB-231 Breast Cancer Cell Lines
by Anelia Mavrova, Stephan Dimov, Inna Sulikovska, Denitsa Yancheva, Ivan Iliev, Iana Tsoneva, Galya Staneva and Biliana Nikolova
Molecules 2022, 27(10), 3314; https://doi.org/10.3390/molecules27103314 - 21 May 2022
Cited by 7 | Viewed by 2354
Abstract
Novel 4-amino-thieno[2,3-d]pyrimidine-6-carboxylates substituted at the second position were prepared by cyclocondensation of 2-amino-3-cyano-thiophene and aryl nitriles in an acidic medium. The design of the target compounds was based on structural optimization. The derivatives thus obtained were tested in vitro against human and mouse [...] Read more.
Novel 4-amino-thieno[2,3-d]pyrimidine-6-carboxylates substituted at the second position were prepared by cyclocondensation of 2-amino-3-cyano-thiophene and aryl nitriles in an acidic medium. The design of the target compounds was based on structural optimization. The derivatives thus obtained were tested in vitro against human and mouse cell lines. The examination of the compound effects on BLAB 3T3 and MFC-10A cells showed that they are safe, making them suitable for subsequent experiments to establish their antitumor activity. The photoirritancy factor of the compounds was calculated. Using the MTT test, the antiproliferative activity to MCF-10A, MCF-7 and MDA-MB-231 cell lines was estimated. The best antiproliferative effect in respect to the MCF-7 cell line revealed compound 2 with IC50 4.3 ± 0.11 µg/mL (0.013 µM). The highest selective index with respect to MCF-7 cells was shown by compound 3 (SI = 19.3), and to MDA-MB-231 cells by compound 2 (SI = 3.7). Based on energy analysis, the most stable conformers were selected and optimized by means of density functional theory (DFT). Ligand efficiency, ligand lipophilicity efficiency and the physicochemical parameters of the target 4-amino-thienopyrimidines were determined. The data obtained indicated that the lead compound among the tested substances is compound 2. Full article
(This article belongs to the Special Issue Synthesis and Biological Evaluation of Novel Drugs as Anticancer Agents)
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14 pages, 3844 KiB  
Article
Design, Synthesis, and Biological Evaluation of Novel MAO-A Inhibitors Targeting Lung Cancer
by Sanaa Bardaweel, Reem Aljanabi, Dima Sabbah and Kamal Sweidan
Molecules 2022, 27(9), 2887; https://doi.org/10.3390/molecules27092887 - 30 Apr 2022
Cited by 17 | Viewed by 3118
Abstract
Lung cancer is one of the most common causes of cancer-related deaths worldwide. Monoamine Oxidase-A (MAO-A) enzyme mediates the production of reactive oxygen species (ROS) that trigger DNA damage and oxidative injury of cells resulting in tumor initiation and progression. Available MAO-A inhibitors [...] Read more.
Lung cancer is one of the most common causes of cancer-related deaths worldwide. Monoamine Oxidase-A (MAO-A) enzyme mediates the production of reactive oxygen species (ROS) that trigger DNA damage and oxidative injury of cells resulting in tumor initiation and progression. Available MAO-A inhibitors are used as antidepressants, however, their role as anticancer agents is still under investigation. Ligand- and structure-based drug design approaches guided the discovery and development of novel MAO-A inhibitors. A series of 1H indole-2-carboxamide derivatives was prepared and characterized using 1H-NMR, 13C-NMR, and IR. The antiproliferative effects of MAO-A inhibitors were evaluated using the cell viability assay (MTT), and MAO-A activity was evaluated using MAO-A activity assay. The presumed inhibitors significantly inhibited the growth of lung cell lines in a dose- and time dependent manner. The half maximal inhibitory concentration (IC50) values of MAO-A inhibitors (S1, S2, S4, S7, and S10) were 33.37, 146.1, 208.99, 307.7, and 147.2 µM, respectively, in A549. Glide docking against MAO-A showed that the derivatives accommodate MAO-A binding cleft and engage with key binding residues. MAO-A inhibitors provide significant and consistent evidence on MAO-A activity in lung cancer and present a potential target for the development of new chemotherapeutic agents. Full article
(This article belongs to the Special Issue Synthesis and Biological Evaluation of Novel Drugs as Anticancer Agents)
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19 pages, 4279 KiB  
Article
Design, Synthesis, and Biological Evaluation of HDAC Degraders with CRBN E3 Ligase Ligands
by Yingxin Lu, Danwen Sun, Donghuai Xiao, Yingying Shao, Mingbo Su, Yubo Zhou, Jia Li, Shulei Zhu and Wei Lu
Molecules 2021, 26(23), 7241; https://doi.org/10.3390/molecules26237241 - 29 Nov 2021
Cited by 15 | Viewed by 4695
Abstract
Histone deacetylases (HDACs) play important roles in cell growth, cell differentiation, cell apoptosis, and many other cellular processes. The inhibition of different classes of HDACs has been shown to be closely related to the therapy of cancers and other diseases. In this study, [...] Read more.
Histone deacetylases (HDACs) play important roles in cell growth, cell differentiation, cell apoptosis, and many other cellular processes. The inhibition of different classes of HDACs has been shown to be closely related to the therapy of cancers and other diseases. In this study, a series of novel CRBN-recruiting HDAC PROTACs were designed and synthesized by linking hydroxamic acid and benzamide with lenalidomide, pomalidomide, and CC-220 through linkers of different lengths and types. One of these PROTACs, denoted 21a, with a new benzyl alcohol linker, exhibited comparably excellent HDAC inhibition activity on different HDAC classes, acceptable degradative activity, and even better in vitro anti-proliferative activities on the MM.1S cell line compared with SAHA. Moreover, we report for the first time the benzyl alcohol linker, which could also offer the potential to be used to develop more types of potent PROTACs for targeting more proteins of interest (POI). Full article
(This article belongs to the Special Issue Synthesis and Biological Evaluation of Novel Drugs as Anticancer Agents)
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11 pages, 2906 KiB  
Article
Design, Synthesis, and Evaluation of Near-Infrared Fluorescent Molecules Based on 4H-1-Benzopyran Core
by Shuting Wang, Shulei Zhu, Yawen Tanzeng, Yuexing Zhang, Chuchu Li, Mingliang Ma and Wei Lu
Molecules 2021, 26(22), 6986; https://doi.org/10.3390/molecules26226986 - 19 Nov 2021
Cited by 1 | Viewed by 2651
Abstract
A series of novel fluorescent 4H-1-benzopyrans was designed and developed as near-infrared fluorescent molecules with a compact donor–acceptor-donor architecture. Spectral intensity of the fluorescent molecules M-1, M-2, M-3 varied significantly with the increasing polarities of solvents, where M-3 showed high viscosity sensitivity in [...] Read more.
A series of novel fluorescent 4H-1-benzopyrans was designed and developed as near-infrared fluorescent molecules with a compact donor–acceptor-donor architecture. Spectral intensity of the fluorescent molecules M-1, M-2, M-3 varied significantly with the increasing polarities of solvents, where M-3 showed high viscosity sensitivity in glycerol-ethanol system with a 3-fold increase in emission intensity. Increasing concentrations of compound M-3 to 5% BSA in PBS elicited a 4-fold increase in fluorescence intensity, exhibiting a superior environmental sensitivity. Furthermore, the in vitro cellular uptake behavior and CLSM assay of cancer cell lines demonstrated that M-3 could easily enter the cell nucleus and bind to proteins with low toxicity. Therefore, the synthesized near-infrared fluorescent molecules could provide a new direction for the development of optical imaging probes and potential further drugs. Full article
(This article belongs to the Special Issue Synthesis and Biological Evaluation of Novel Drugs as Anticancer Agents)
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