Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	2-Cyclopropanecarboxamido- 6-carboxamide substituted benzothiazoles: Synthesis, in vitro and in vivo evaluation of their antiproliferative and anti-tumorigenic activity
Δημιουργός/Συγγραφέας:	Batsi, Yakinthi [EL] Αντωνοπούλου, Γεωργία[EN] Antonopoulou, Georgia Galatis-Vaxovanos, Constantinos Goulielmaki, Maria Koumaki, Kassandra Papalouka, Chara Poulou-Sidiropoulou, Eleni [EL] Κοσμίδου, Παρασκευή[EN] Kosmidou, Paraskevi Vidali, Maria-Sofia Kritsi, Eftichia Potamitis, Constantinos Douna, Stavroula Gkotsi, Eleni-Fani [EL] Μαγουλάς, Γιώργος[EN] Magoulas, George [EL] Χατζηιωάννου, Αριστοτέλης[EN] Chatziioannou, Aristotelis [EL] Σουλιώτης, Βασίλης Λ.[EN] Souliotis, Vassilis L. [EL] Πλέτσα, Βασιλική[EN] Pletsa, Vassiliki [EL] Παπαδόδημα, Όλγα[EN] Papadodima, Olga [EL] Ζουμπουρλής, Βασίλης[EN] Zoumpourlis, Vassilis [EL] Ζερβού, Μαρία[EN] Zervou, Maria [EL] Γεωργιάδης, Παναγιώτης[EN] Georgiadis, Panagiotis [EL] Πίντζας, Αλέξανδρος[EN] Pintzas, Alexander [EL] Κώστας, Ιωάννης Δ.[EN] Kostas, Ioannis D.
Ημερομηνία:	2025-10-16
Γλώσσα:	Αγγλικά
ISSN:	09680896
DOI:	10.1016/j.bmc.2025.118450
Άλλο:	41135285
Περίληψη:	To expand our structure-activity relationship studies exploiting substituted benzothiazoles as potential antiproliferative and antitumor agents, we developed a new class of benzothiazole derivatives by coupling of 2-(cyclopropanecarboxamido)benzo[d]thiazole-6-carboxylic acid with a series of amines. All synthesized compounds bear a cyclopropanecarboxamido- moiety and a carboxamide functionality anchored to the positions C-2 and C-6 of the benzothiazole scaffold, respectively. Furthermore, the carboxamide was used as a handle for further derivatization using linkers with variability in length and conformation. The antiproliferative and antitumor activity of the compounds was assessed in various colorectal cancer and melanoma cell lines and several cancer cell lines generated from other tissues (hepatocyte carcinoma, prostate adenocarcinoma, breast adenocarcinoma, osteosarcoma, lung carcinoma, and adult acute monocytic leukemia). In all cell viability experiments, two analogs showed promising activity and, therefore, their effects were further investigated on the global gene expression of colorectal cell lines. In particular, treatment with the derivative 2-(cyclopropanecarboxamido)-N-[2-(phenylsulfonamido)ethylene]benzo[d]thiazole-6-carboxamide had the greatest influence on gene expression. Cancer-related biological processes were drastically affected, including nucleosome and chromatin assembly, cell cycle, p53 signal transduction and apoptosis. Both analogs were also evaluated in vivo in mice bearing a colon cancer xenograft model, demonstrating significant anticancer activity.
Τίτλος πηγής δημοσίευσης:	Bioorganic & medicinal chemistry
Τόμος/Κεφάλαιο:	132
Θεματική Κατηγορία:	[EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry [EL] Οργανική χημεία[EN] Organic chemistry [EL] Νεοπλάσματα. Όγκοι. Ογκολογία (περ. Καρκίνος, κακινογόνες ουσίες)[EN] Neoplasms. Tumors. Oncology (Incl.cancer, carcinogens) [EL] Μοριακή Βιολογία[EN] Molecular Biology [EL] Κυτταρολογία[EN] Cytology
Λέξεις-Κλειδιά:	Apoptosis Benzothiazole Cancer Colon cancer cells In vitro biological evaluation In vivo bioassays Melanoma cancer cells
Χρηματοδότης:	European Regional Development Fund University of Crete, Medical School National Hellenic Research Foundation, Institute of Chemical Biology
Χρηματοδοτικό πρόγραμμα:	STHENOS-b EATRIS-GR Strengthening Human Resources Research Potential via Doctorate Research Oncology: from Oncogenesis to Therapy
Αναγνωριστικό χρηματοδοτικού προγράμματος:	MIS 5002398 MIS 5028091 MIS-5000432
Κάτοχος πνευματικών δικαιωμάτων:	© 2025 Elsevier Ltd. All rights are reserved, including those for text and data mining, AI training, and similar technologies.
Ηλεκτρονική διεύθυνση στον εκδότη (link):	https://doi.org/10.1016/j.bmc.2025.118450
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο