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Medicinal Chemistry in China II
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Medicinal Chemistry in China II

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

Deadline for manuscript submissions: closed (31 October 2023) | Viewed by 6432

Special Issue Editors

Prof. Dr. Jiang Wang

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Guest Editor
State Key Laboratory of Drug Research, Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China
Interests: medicinal chemistry; drug design; discovery and development of metabolic novel drug; lead compound discovery and optimization; high efficient synthetic methodology; non-natural amino acid
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Liang-Ren Zhang

E-Mail Website
Guest Editor
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
Interests: nucleosides and nucleotides; drug design and synthesis; molecular modeling
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Peng Zhan

E-Mail Website
Guest Editor
Key Laboratory of Chemical Biology (Ministry of Education), Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 Wenhuaxi Road, Ji'nan 250012, China
Interests: antiviral drug; medicinal chemistry; drug design; new drug modalities
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Tian-Miao Ou

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Guest Editor
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China
Interests: telomere; DNA; senescence; cancer biology; genome stability; molecular cell biology; RNA
Special Issues, Collections and Topics in MDPI journals
Dr. Lei Wang

E-Mail Website
Guest Editor
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
Interests: anticancer agents; molecular chaperones; small molecules; protein-protein interactions; computer-aided drug design

Special Issue Information

Dear Colleagues,

This Special Issue is entitled “Medicinal Chemistry in China II”. In China, many research groups, both from industry and academia, are working on medicinal chemistry topics that cover almost all therapeutic fields, ranging from metabolic disease, CNS disease, anticancer agents, and antiviral agents. Molecules devoted to the treatment of rare disease are also being investigated. The results obtained, frequently very important and recognized all over the world, are derived from the close collaboration of experts in different areas, such as computational chemistry, organic chemistry, biology, biochemistry, and pharmacology.

Scientists from China are cordially invited to contribute original research papers or reviews to this Special Issue of Molecules, which reports on the design, synthesis, and biological evaluation of potentially active compounds in the different subjects of medicinal chemistry.

Prof. Dr. Jiang Wang
Prof. Dr. Liang-Ren Zhang
Prof. Dr. Peng Zhan
Prof. Dr. Tian-Miao Ou
Dr. Lei Wang
Guest Editors

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 submissions that pass pre-check are 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 2700 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

  • drug design
  • drug discovery
  • lead compounds
  • anticancer agents
  • antiviral agents
  • antidiabetic agents
  • CNS agents

Published Papers (4 papers)

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Research

18 pages, 4053 KiB  
Article
Development of Hydroxamate Derivatives Containing a Pyrazoline Moiety as APN Inhibitors to Overcome Angiogenesis
by Yangyang Liu, Dongsheng Zhao, Chenghua Zhang, Hui Fang, Qingsitong Shen, Zhixian Wang and Jiangying Cao
Molecules 2022, 27(23), 8339; https://doi.org/10.3390/molecules27238339 - 29 Nov 2022
Viewed by 1151
Abstract
Aminopeptidase N (APN) was closely associated with cancer invasion, metastasis, and angiogenesis. Therefore, APN inhibitors have attracted more and more attention of scientists as antitumor agents. In the current study, we designed, synthesized, and evaluated one new series of pyrazoline-based hydroxamate derivatives as [...] Read more.
Aminopeptidase N (APN) was closely associated with cancer invasion, metastasis, and angiogenesis. Therefore, APN inhibitors have attracted more and more attention of scientists as antitumor agents. In the current study, we designed, synthesized, and evaluated one new series of pyrazoline-based hydroxamate derivatives as APN inhibitors. Moreover, the structure–activity relationships of those were discussed in detail. 2,6-Dichloro substituted compound 14o with R1 = CH3, showed the best capacity for inhibiting APN with an IC50 value of 0.0062 ± 0.0004 μM, which was three orders of magnitude better than that of the positive control bestatin. Compound 14o possessed both potent anti-proliferative activities against tumor cells and potent anti-angiogenic activity. At the same concentration of 50 μM, compound 14o exhibited much better capacity for inhibiting the micro-vessel growth relative to bestatin in the rat thoracic aorta ring model. Additionally, the putative interactions of 14o with the active site of APN are also discussed. The hydroxamate moiety chelated the zinc ion and formed four hydrogen bonds with His297, Glu298 and His301. Meanwhile, the terminal phenyl group and another phenyl group of 14o interacted with S2′ and S1 pockets via hydrophobic effects, respectively. Full article
(This article belongs to the Special Issue Medicinal Chemistry in China II)
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10 pages, 2384 KiB  
Article
(20S) Ginsenoside Rh2-Activated, Distinct Apoptosis Pathways in Highly and Poorly Differentiated Human Esophageal Cancer Cells
by He Li, Chunxiao Han, Chen Chen, Guanghong Han and Yang Li
Molecules 2022, 27(17), 5602; https://doi.org/10.3390/molecules27175602 - 31 Aug 2022
Cited by 1 | Viewed by 1390
Abstract
Ginsenoside Rh2 (G-Rh2), a rare ginsenoside isolated from red ginseng, has considerable anti-cancer activity and induces apoptosis in a variety of cancer cells, but its activity in esophageal cancer cells is unclear. In this study, we examined the cytotoxic activity of (20S) G-Rh2 [...] Read more.
Ginsenoside Rh2 (G-Rh2), a rare ginsenoside isolated from red ginseng, has considerable anti-cancer activity and induces apoptosis in a variety of cancer cells, but its activity in esophageal cancer cells is unclear. In this study, we examined the cytotoxic activity of (20S) G-Rh2 in highly differentiated esophageal squamous ECA109 cells and poorly differentiated esophageal squamous TE-13 cells. (20S) G-Rh2 exerted intense cytotoxicity in ECA109 and TE-13 cells with an IC50 of 2.9 and 3.7 μg/mL, respectively. After treatment with G-Rh2, Bcl-2, and Bcl-xL, the two main anti-apoptosis Bcl-2 family proteins upregulated, and Bax and Bak, the two key pro-apoptosis proteins translocated to mitochondria in both cell lines. At the same time, cytochrome c and Smac released from mitochondria, followed by caspase-9 activation, indicating that a mitochondria-mediated intrinsic apoptosis pathway was activated in both cell lines upon treatment with (20S) G-Rh2. It is noteworthy that (20S) G-Rh2 upregulated the transcription and protein expression of two death receptors, Fas and DR5, and subsequently activated Caspase-8 in the TE-13 cells but not in the ECA109 cells. Taken together, we demonstrated the potent anti-esophageal cancer cell activity of (20S) G-Rh2 and showed its working mechanism in two differentiated esophageal cancer cells, which can provide important evidence for developing an effective strategy for anti-esophageal cancer treatment. Full article
(This article belongs to the Special Issue Medicinal Chemistry in China II)
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12 pages, 2981 KiB  
Article
Super Early Scan of PSMA PET/CT in Evaluating Primary and Metastatic Lesions of Prostate Cancer
by Juanli Mao, Mingjun Gao, Bin Cui, Yingying Zhang, Xiaojiao Wang, Siyu Liang, Changjing Zuo, Peng Chen and Aisheng Dong
Molecules 2022, 27(14), 4661; https://doi.org/10.3390/molecules27144661 - 21 Jul 2022
Viewed by 1551
Abstract
68Ga-prostate specific membrane antigen (PSMA)-11 PET/CT has been widely used in the diagnosis of prostate cancer (PCa); however, the urine lead shielding resulting from the urinary metabolism of tracers may obstruct the detection of surrounding metastasis. In this research, the additive value [...] Read more.
68Ga-prostate specific membrane antigen (PSMA)-11 PET/CT has been widely used in the diagnosis of prostate cancer (PCa); however, the urine lead shielding resulting from the urinary metabolism of tracers may obstruct the detection of surrounding metastasis. In this research, the additive value of super early scanning in diagnosing primary lesions and metastasis in the pelvic cavity was evaluated. Firstly, the differentiation efficiency of 68Ga-PSMA-11 PET scanned at 3 min post-injection (min P.I.) was measured in PSMA-positive (22rv1 cells) and PSMA-negative (PC3 cells) model mice. Secondly, 106 patients were scanned at 3 min P.I. for the pelvic cavity and then scanned as a standard protocol at 45 min P.I. In the results, the differential diagnosis of PSMA expression was completely reflected as early as 3 min P.I. for mice models. For patients, when correlated with the Gleason score, the quantitative results of the super early scan displayed a comparable correlation coefficient with the routine scan. The target to bladder ratios increased from 1.44 ± 2.40 at 45 min to 10.10 ± 19.10 at 3 min (p < 0.001) for the primary lesions, and it increased from 0.99 ± 1.88 to 9.27 ± 23.03 for metastasis. Meanwhile, the target to background ratios increased from 2.21 ± 2.44 at 3 min to 19.13 ± 23.93 at 45 min (p < 0.001) for the primary lesions, and it increased from 1.68 ± 2.71 to 12.04 ± 18.73 (p < 0.001) for metastasis. In conclusion, super early scanning of 68Ga-PSMA-11 PET/CT added referable information for metastasis detection in order to avoid disturbing tracer activity in the urinary system. Full article
(This article belongs to the Special Issue Medicinal Chemistry in China II)
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14 pages, 2446 KiB  
Article
A Novel Strategy for Regulating mRNA’s Degradation via Interfering the AUF1’s Binding to mRNA
by Kun-Tao Li, Xiong-Zhi Wu, Zhi-Yin Sun and Tian-Miao Ou
Molecules 2022, 27(10), 3182; https://doi.org/10.3390/molecules27103182 - 16 May 2022
Cited by 1 | Viewed by 1681
Abstract
The study on the mechanism and kinetics of mRNA degradation provides a new vision for chemical intervention on protein expression. The AU enrichment element (ARE) in mRNA 3′-UTR can be recognized and bound by the ARE binding protein (AU-rich Element factor (AUF1) to [...] Read more.
The study on the mechanism and kinetics of mRNA degradation provides a new vision for chemical intervention on protein expression. The AU enrichment element (ARE) in mRNA 3′-UTR can be recognized and bound by the ARE binding protein (AU-rich Element factor (AUF1) to recruit RNase for degradation. In the present study, we proposed a novel strategy for expression regulation that interferes with the AUF1-RNA binding. A small-molecule compound, JNJ-7706621, was found to bind AUF1 protein and inhibit mRNA degradation by screening the commercial compound library. We discovered that JNJ-7706621 could inhibit the expression of AUF1 targeted gene IL8, an essential pro-inflammatory factor, by interfering with the mRNA homeostatic state. These studies provide innovative drug design strategies to regulate mRNA homeostasis. Full article
(This article belongs to the Special Issue Medicinal Chemistry in China II)
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