Εξειδίκευση τύπου :	Άρθρο σε περιοδικό τύπο
Τίτλος:	Development of a multigram synthesis of the bradykinin receptor 2 agonist FR-190997 and analogs thereof
Δημιουργός/Συγγραφέας:	Vachlioti, Eleanna Ferikoglou, Spyridon Georgiou, Xenios Karampatsis, Vasilios Afratis, Konstantinos Bafiti, Vivi Savard, Martin Papaioannou, Dionissios [EL] Κατσίλα, Θεοδώρα[EN] Katsila, Theodora Gobeil, Fernand Rassias, Gerasimos
Ημερομηνία:	2023-05
Γλώσσα:	Αγγλικά
ISSN:	0365-6233 1521-4184
DOI:	10.1002/ardp.202200610
Άλλο:	36720040
Περίληψη:	Using Fujisawa's B2R agonist FR-190997, we recently demonstrated for the first time that agonism at the bradykinin receptor type 2 (B2R) produces substantial antiproliferative effects. FR-190997 elicited an EC50 of 80 nM in the triple-negative breast cancer cell line MDA-MB-231, a much superior performance to that exhibited by most approved breast cancer drugs. Consequently, we initiated a program aiming primarily at synthesizing adequate quantities of FR-190997 to support further in vitro and in vivo studies toward its repurposing for various cancers and, in parallel, enable the generation of novel FR-190997 analogs for an SAR study. Prerequisite for this endeavor was to address the synthetic challenges associated with the FR-190997 scaffold, which the Fujisawa chemists had constructed in 20 steps, 13 of which required chromatographic purification. We succeeded in developing a 17-step synthesis amenable to late-stage diversification that eliminated all chromatography and enabled access to multigram quantities of FR-190997 and novel derivatives thereof, supporting further anticancer research based on B2R agonists.
Τίτλος πηγής δημοσίευσης:	Archiv der Pharmazie
Τόμος/Κεφάλαιο:	356
Τεύχος:	5
Θεματική Κατηγορία:	[EL] Θεραπευτική. Φαρμακολογία[EN] Therapeutics.Pharmacology [EL] Νεοπλάσματα. Όγκοι. Ογκολογία (περ. Καρκίνος, κακινογόνες ουσίες)[EN] Neoplasms. Tumors. Oncology (Incl.cancer, carcinogens) [EL] Κυτταρολογία[EN] Cytology [EL] Φαρμακευτική χημεία[EN] Pharmaceutical chemistry
Λέξεις-Κλειδιά:	B2R agonists FR-190997 cancer late-stage diversification quinolines
Κάτοχος πνευματικών δικαιωμάτων:	© 2023 The Authors. Archiv der Pharmazie published by Wiley-VCH GmbH on behalf of Deutsche Pharmazeutische Gesellschaft.
Ηλεκτρονική διεύθυνση στον εκδότη (link):	https://doi.org/10.1002/ardp.202200610
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο