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Curcumin-1,2,3-Triazole Conjugation for Targeting the Cancer Apoptosis Machinery

Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
Department for Life Quality Studies, Alma Mater Studiorum-University of Bologna, Corso d’Augusto 237, 47921 Rimini, Italy
Department of Biomolecular Sciences, University of Urbino Carlo Bo, Via Ca’ Le Suore, 2, 61029 Urbino, Italy
Cell Death Investigation and Therapy Laboratory, Department of Human Structure and Repair, Ghent University, 9000 Ghent, Belgium
Cancer Research Institute Ghent, 9000 Ghent, Belgium
Department of Pathophysiology, Sechenov First Moscow State Medical University (Sechenov University), 119146 Moscow, Russia
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Present address: Department of Drug Discovery and Development, Istituto Italiano di Tecnologia, via Morego n. 30, 16163 Genova, Italy.
Academic Editor: M. Helena Vasconcelos
Molecules 2020, 25(13), 3066;
Received: 27 May 2020 / Revised: 25 June 2020 / Accepted: 2 July 2020 / Published: 5 July 2020
The burden of neoplastic diseases is widely recognized as a severe cause of mortality. The clinical inadequacy of most anticancer therapeutics urgently prompted intense drug discovery efforts toward the identification of new chemical entities endowed with a potent and safe antitumor profile. In this scenario, targeting cancer cells apoptosis machinery has emerged as a relevant strategy, useful for tackling the emergence of drug resistance. On this basis, a small library of naturally inspired hybrid molecules was obtained by combining, through a click chemistry approach, “privileged” synthons such as curcumin scaffold and 1,2,3-triazole building block. Compound 1, bearing a para-fluoro phenyl moiety, showed low-micromolar potency against T acute lymphoblastic leukemia cell growth. More in-depth biologic studies demonstrated, for this analog, cell death-inducing properties associated with its capability to simultaneously activate both the receptor and the mitochondrial apoptosis cascades. This peculiar behavior offers promises for achieving an expanded anticancer effect, namely intense cytotoxic response coupled with reduced predisposition of chemoresistance insurgence. Altogether, this study allowed the identification of compound 1 as a lead compound worth to be progressed as an anticancer drug candidate. View Full-Text
Keywords: apoptosis; cell cycle; cell death; click chemistry; curcumin; flow cytometry; fluorine; privileged structure; triazole apoptosis; cell cycle; cell death; click chemistry; curcumin; flow cytometry; fluorine; privileged structure; triazole
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MDPI and ACS Style

Seghetti, F.; Di Martino, R.M.C.; Catanzaro, E.; Bisi, A.; Gobbi, S.; Rampa, A.; Canonico, B.; Montanari, M.; Krysko, D.V.; Papa, S.; Fimognari, C.; Belluti, F. Curcumin-1,2,3-Triazole Conjugation for Targeting the Cancer Apoptosis Machinery. Molecules 2020, 25, 3066.

AMA Style

Seghetti F, Di Martino RMC, Catanzaro E, Bisi A, Gobbi S, Rampa A, Canonico B, Montanari M, Krysko DV, Papa S, Fimognari C, Belluti F. Curcumin-1,2,3-Triazole Conjugation for Targeting the Cancer Apoptosis Machinery. Molecules. 2020; 25(13):3066.

Chicago/Turabian Style

Seghetti, Francesca, Rita M.C. Di Martino, Elena Catanzaro, Alessandra Bisi, Silvia Gobbi, Angela Rampa, Barbara Canonico, Mariele Montanari, Dmitri V. Krysko, Stefano Papa, Carmela Fimognari, and Federica Belluti. 2020. "Curcumin-1,2,3-Triazole Conjugation for Targeting the Cancer Apoptosis Machinery" Molecules 25, no. 13: 3066.

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