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Molecules, Vol. 28, Pages 6329: From Monoamine Oxidase Inhibition to Antiproliferative Activity: New Biological Perspectives for Polyamine Analogs
Maria Luisa Di Paolo Monoamine oxidases (MAOs) are well-known pharmacological targets in neurological and neurodegenerative diseases. However, recent studies have revealed a new role for MAOs in certain types of cancer such as glioblastoma and prostate cancer, in which they have been found overexpressed. This finding is opening new frontiers for MAO inhibitors as potential antiproliferative agents. In light of our previous studies demonstrating how a polyamine scaffold can act as MAO inhibitor, our aim was to search for novel analogs with greater inhibitory potency for human MAOs and possibly with antiproliferative ac...
Source: Molecules - August 29, 2023 Category: Chemistry Authors: Giulia Nordio Francesco Piazzola Giorgio Cozza Monica Rossetto Manuela Cervelli Anna Minarini Filippo Basagni Elisa Tassinari Lisa Dalla Via Andrea Milelli Maria Luisa Di Paolo Tags: Article Source Type: research

Molecules, Vol. 28, Pages 3959: Cytotoxic Activity, Topoisomerase I Inhibition and In Silico Studies of New Sesquiterpene-aryl Ester Derivatives of (-) Drimenol
In this study, we aimed to evaluate two sets of sesquiterpene-aryl derivatives linked by an ester bond, their cytotoxic activities, and their capacity to activate caspases 3/7 and inhibit human topoisomerase I (TOP1). A total of 13 compounds were synthesized from the natural sesquiterpene (-)-drimenol and their cytotoxic activity was evaluated in vitro against three cancer cell lines: PC-3 (prostate cancer), HT-29 (colon cancer), MCF-7 (breast cancer), and an immortalized non-tumoral cell line (MCF-10). From the results, it was observed that 6a was the most promising compound due to its cytotoxic effect on three cancer cel...
Source: Molecules - May 8, 2023 Category: Chemistry Authors: Ileana Araque Javiera Ram írez Rut Vergara Jaime Mella Pablo Ar ánguiz Luis Espinoza Waleska Vera Iv án Montenegro Cristian O. Salas Joan Villena Mauricio A. Cuellar Tags: Article Source Type: research

Molecules, Vol. 26, Pages 6421: 3-O-Carbamoyl-5,7,20-O-trimethylsilybins: Synthesis and Preliminary Antiproliferative Evaluation
Hong Chen 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 cel...
Source: Molecules - October 24, 2021 Category: Chemistry Authors: Sitong Wu Guanglin Chen Qiang Zhang Guangdi Wang Qiao-Hong Chen Tags: Article Source Type: research

Molecules, Vol. 26, Pages 6142: Caryophyllene Oxide, the Active Compound Isolated from Leaves of Hymenaea courbaril L. (Fabaceae) with Antiproliferative and Apoptotic Effects on PC-3 Androgen-Independent Prostate Cancer Cell Line
Celis Cancer treatment frequently carries side effects, therefore, the search for new selective and effective molecules is indispensable. Hymenaea courbaril L. has been used in traditional medicine in South America to treat several diseases, including prostate cancer. Leaves’ extracts from different polarities were evaluated using the 3-(4,5-methyl-thiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) cell viability assay to determine the cytotoxicity in prostate p53-null cells, followed by bio-guided fractionations to obtain the most cytotoxic fraction considering the selectivity index. The most cytotoxic fraction wa...
Source: Molecules - October 12, 2021 Category: Chemistry Authors: Claudia Delgado Gina Mendez-Callejas Crispin Celis Tags: Article Source Type: research

Molecules, Vol. 24, Pages 1393: Curcumin: Total-Scale Analysis of the Scientific Literature
gozliev Karel Šmejkal Atanas G. Atanasov The current study aimed to provide a comprehensive bibliometric overview of the literature on curcumin, complementing the previous reviews and meta-analyses on its potential health benefits. Bibliometric data for the current analysis were extracted from the Web of Science Core Collection database, using the search string TOPIC=(“curcumin*”), and analyzed by the VOSviewer software. The search yielded 18,036 manuscripts. The ratio of original articles to reviews was 10.4:1. More than half of the papers have been published since 2014. The major cont...
Source: Molecules - April 8, 2019 Category: Chemistry Authors: Andy Wai Kan Yeung Michal Horba ńczuk Nikolay T. Tzvetkov Andrei Mocan Simone Carradori Filippo Maggi Joanna Marchewka Stefania Sut Stefano Dall ’Acqua Ren-You Gan Lyubka P. Tancheva Timea Polgar Ioana Berindan-Neagoe Vasil Pirgozliev Karel Šmejkal At Tags: Article Source Type: research

Molecules, Vol. 23, Pages 567: Identification and Characterizations of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Scaffold Hopping- and 2D-Molecular Fingerprint-Based Similarity Search
heng Luo Kai Chen SET7, serving as the only histone methyltransferase that monomethylates ‘Lys-4’ of histone H3, has been proved to function as a key regulator in diverse biological processes, such as cell proliferation, transcriptional network regulation in embryonic stem cell, cell cycle control, protein stability, heart morphogenesis and development. What′s more, SET7 is involved inthe pathogenesis of alopecia aerate, breast cancer, tumor and cancer progression, atherosclerosis in human carotid plaques, chronic renal diseases, diabetes, obesity, ovarian cancer, prostate cancer, hepatocellular carcinoma, and ...
Source: Molecules - March 2, 2018 Category: Chemistry Authors: Hong Ding Wen Lu Jun Hu Yu-Chih Liu Chen Zhang Fu Lian Nai Zhang Fan Meng Cheng Luo Kai Chen Tags: Article Source Type: research

Molecules, Vol. 22, Pages 1680: Natriuretic Peptides: The Case of Prostate Cancer
ellezza Cardiac natriuretic peptides have long been known to act as main players in the homeostatic control of blood pressure, salt and water balance. However, in the last few decades, new properties have been ascribed to these hormones. A systematic review of English articles using MEDLINE Search terms included prostate cancer, inflammation, cardiac hormones, atrial natriuretic peptide, and brain natriuretic peptide. Most recent publications were selected. Natriuretic peptides are strongly connected to the immune system, whose two branches, innate and adaptive, are finely tuned and organized to kill invaders and repai...
Source: Molecules - October 10, 2017 Category: Chemistry Authors: Letizia Mezzasoma Matthew Peirce Alba Minelli Ilaria Bellezza Tags: Review Source Type: research