Culicinin D is a 10 amino acid peptaibol containing a rare and synthetically challenging (2S,4S,6R)-AHMOD residue, that exhibits potent antiproliferative activity against MDA-MB-468 cells. An SAR study focusing on replacement of the AHMOD residue was undertaken, culminating in the revelation that a 6-hydroxy or 6-keto substituent was essential to retain potent low nanomolar antiproliferative activity.
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http://dx.doi.org/10.1016/j.ejmech.2019.05.052 | DOI Listing |
Int J Mol Sci
January 2025
School of Applied Sciences, College of Health, Science and Society, University of the West of England, Coldharbour Lane, Bristol BS16 1QY, UK.
The active metabolite of vitamin D3, calcitriol (1,25D), is widely recognised for its direct anti-proliferative and pro-differentiation effects. However, 1,25D is calcaemic, which restricts its clinical use for cancer treatment. Non-calcaemic agonists of the vitamin D receptor (VDR) could be better candidates for cancer treatment.
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December 2024
Department of Biomedical Sciences, School of Medicine Nazarbayev University, Astana 010000, Kazakhstan.
Metformin is an antidiabetic drug with reported potential antiproliferative activity against different cancer types including breast cancer. However, the mechanism of action of how metformin can induce its antiproliferative activity is still unclear. Thus, the current study is a systematic review of the literature aiming to explore the reported antiproliferative mechanisms of metformin against breast cancer.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Pharmacy, University of Naples Federico II, 80131 Napoli, Italy.
Thrombin binding aptamer (TBA) is one of the best-known G-quadruplex (G4)-forming aptamers that efficiently binds to thrombin, resulting in anticoagulant effects. TBA also possesses promising antiproliferative properties. As with most therapeutic oligonucleotides, chemical modifications are critical for therapeutic applications, particularly to improve thermodynamic stability, resistance in biological environment, and target affinity.
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January 2025
Engineering Research Center of Tropical Medicine Innovation and Transformation of Ministry of Education, International Joint Research Center of Human-Machine Intelligent Collaborative for Tumor Precision Diagnosis and Treatment of Hainan Province, Hainan Provincial Key Laboratory of Research and Development on Tropical Herbs, School of Pharmaceutical Sciences, Hainan Medical University, Haikou 571199, China.
An efficient Rh(III)-catalyzed C-H activation of azobenzenes and subsequent [4+1] cascade annulation with CF-imidoyl sulfoxonium ylides was developed, yielding diverse CF-indazoles. This protocol featured easily available starting materials, excellent functional group tolerance and high efficiency. Moreover, the antitumor activities of selected CF-indazoles against human cancer cell lines were also studied, and the results indicated that several compounds displayed considerable antiproliferative activities.
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January 2025
Department of Pharmacy, Jilin Medical University, Jilin 132013, China.
An efficient stereoselective synthesis of 10-hydroxy-10-(1-indol-3-yl)-9-(10)-phenanthrene derivatives was realized through an organocatalyzed Friedel-Crafts reaction of phenanthrenequinones and indoles using a (,)-dimethylaminocyclohexyl-squaramide as the catalyst. Under the optimized conditions, the desired chiral products were obtained in good yields (73-90%) with moderate to high ee values (up to 97% ee). Two pairs of synthesized enantiomers were subjected to evaluation of their antiproliferative activities on four types of human cancer cell lines and one human umbilical vein endothelial cell line using the CCK-8 assay.
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