Article
Biochemistry & Molecular Biology
Wei Ju, Na Li, Junjie Wang, Nairong Yu, Zhichao Lei, Lulu Zhang, Jianbo Sun, Li Chen
Summary: This study improved the mitochondrial-targeting ability and selectivity of CDDO derivatives by linking triphenyl-phosphine cations or tricyclohexylphosphine cations. The new compound 5b showed greater activity against tumor cells than existing CDDO derivatives, causing apoptosis mainly through the mitochondria-mediated intrinsic pathway.
BIOORGANIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Nabil A. Alhakamy, Mohammad Saquib, Sanobar, Mohammad Faheem Khan, Waseem Ahmad Ansari, Deema O. Arif, Mohammad Irfan, Mohammad Imran Khan, Mohd Kamil Hussain
Summary: Twelve novel compounds were synthesized and evaluated for their anticancer activity against breast cancer cells, with one compound showing stronger activity than the standard drug.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Weihong Lai, Jiaxin Chen, Xinjiao Gao, Xiaobao Jin, Gong Chen, Lianbao Ye
Summary: A novel chalcone derivative, A14, was discovered to have excellent antiproliferative activity against breast cancer cells. A14 could inhibit the proliferation and colony formation activity of MCF-7 cells, making it a promising compound for further anti-breast cancer research.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Valentina Albanese, Sonia Missiroli, Mariasole Perrone, Martina Fabbri, Caterina Boncompagni, Salvatore Pacifico, Tiziano De Ventura, Antonella Ciancetta, Giulio Dondio, Franz Kricek, Paolo Pinton, Remo Guerrini, Delia Preti, Carlotta Giorgi
Summary: A series of aryl sulfonamide derivatives (ASDs) were designed and synthesized to inhibit the activation of the NLRP3 inflammasome. Compounds 6c, 7n, and 10 specifically inhibited NLRP3 activation at nanomolar concentrations without affecting the activation of other inflammasomes. These compounds were also found to reduce IL-1 beta production in vivo and attenuate melanoma tumor growth. The findings suggest that these potent NLRP3 inflammasome inhibitors could be considered for future therapeutic approaches in NLRP3 inflammasome-driven cancer.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Blazej Grodner, Mariola Napiorkowska, Dariusz Maciej Pisklak
Summary: This study investigates the type and inhibitory strength of catalase using two pairs of aminoalkanol derivatives. The results show that all four derivatives are competitive inhibitors of catalase, but their strength of action depends on the type of substituents present in the molecule's main structure. The study also demonstrates the weak inhibitory strength of these derivatives through docking studies and analysis of kinetic parameters.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Francisco Estevez-Sarmiento, Ester Saavedra, Ignacio Brouard, Jesus Peyrac, Judith Hernandez-Garces, Celina Garcia, Jose Quintana, Francisco Estevez
Summary: This study investigated the effects of synthetic guanidines on human cancer cells and found that one compound showed the highest cytotoxicity. It was effective against leukemia cells and melanoma cells, with low cytotoxicity against normal cells. These synthetic guanidines may be useful in developing new strategies against cancer.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Robert Pluskota, Karol Jaroch, Piotr Koslinski, Blanka Ziomkowska, Agnieszka Lewinska, Stefan Kruszewski, Barbara Bojko, Marcin Koba
Summary: The synthesis of antiproliferative 2-arylidene-indan-1,3-dione derivatives with potential pharmaceutical applications was presented. These compounds showed strong binding to albumin, met Lipinski's and Veber's rule, and thus could be considered as good candidates for drug development.
Article
Biochemistry & Molecular Biology
Andre Gustavo Tempone, Reinaldo dos Santos Theodoro, Maiara Maria Romanelli, Dayana Agnes Santos Ferreira, Maiara Amaral, Leticia Ribeiro de Assis, Lucas Monteiro Santa Cruz, Alan Roberto Costa, Rosemeire Cobo Zanella, Myron Christodoulides, Luis Octavio Regasini, Carlos Henrique Camargo
Summary: The emergence and spread of multidrug-resistant enterococci and other Gram-positive bacteria is a severe problem, and natural products can provide new antibacterial scaffolds to combat the current antibiotic crisis. A fully synthetic chalcone derivative, r4MB, has been found to exhibit strong antimicrobial activity against multidrug-resistant enterococci and does not show cytotoxicity.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Biochemistry & Molecular Biology
Viviana Poliseno, Silvia Chaves, Leonardo Brunetti, Fulvio Loiodice, Antonio Carrieri, Antonio Laghezza, Paolo Tortorella, Joao D. Magalhaes, Sandra M. Cardoso, M. Amelia Santos, Luca Piemontese
Summary: Alzheimer's disease is a multifactorial neurodegenerative pathology with increasing societal impact. Tenuazonic acid has been identified as a potential multitarget ligand with promising anti-AD properties. Synthesized derivatives of tenuazonic acid showed activity against selected targets and one compound exhibited good chelating ability towards metal ions. These findings suggest tenuazonic acid as a potential building block for innovative anti-neurodegenerative drugs, with specific compounds showing non-cytotoxicity and protective effects in neuroblastoma cells.
Article
Chemistry, Medicinal
Yichao Wan, Guoqing Fang, Hongjuan Chen, Xu Deng, Zilong Tang
Summary: This review summarizes recent advances of sulfonamide derivatives as potential anti-cancer agents, focusing on their applications on anti-cancer targets and corresponding structure-activity relationships.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Amit Kumar Tripathi, Jamboor K. Vishwanatha
Summary: The use of peptide-based drugs for cancer treatment is becoming more significant in the pharmaceutical industry. Anticancer peptides with immunomodulatory activity could be key lead molecules in designing effective cancer therapeutics.
Article
Biochemistry & Molecular Biology
Raimundo de A. M. Neto, Cleydson B. R. Santos, Shayanne V. C. Henriques, Leticia de O. Machado, Jorddy N. Cruz, Carlos H. T. de P. da Silva, Leonardo B. Federico, Edivaldo H. C. de Oliveira, Michel P. C. de Souza, Patricia N. B. da Silva, Carlton A. Taft, Irlon M. Ferreira, Madson R. F. Gomes
Summary: This study evaluated the antineoplastic activity of synthetic chalcones in glioblastoma models, showing that these compounds can significantly reduce the viability of tumor cells and interact with serine and lysine amino acids, suggesting potential for inhibiting tumor growth. Molecular dynamics studies were also conducted to investigate the binding mechanism of these compounds with tubulin.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Medicinal
Yiyue Feng, Yingmei Lu, Junfang Li, Honghua Zhang, Zhao Li, Hanzhong Feng, Xuemei Deng, Dan Liu, Tao Shi, Weifan Jiang, Yongxing He, Jian Zhang, Zhen Wang
Summary: By designing and synthesizing o-aminobenzamide derivatives, compounds F8 and T9 were identified as potent anti-gastric cancer agents, with F8 showing better efficacy and lower toxicity in vivo.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Snehal A. Arvindekar, Suraj Mohole, Aishwarya Patil, Pradnya Mane, Aditya Arvindekar, Suraj N. Mali, Bapu Thorat, Ravi Rawat, Shilpa Sharma
Summary: This study aimed to design and synthesize a series of benzopyran-chalcones as potential anti-breast cancer agents. The synthesized compounds showed activity against ER+MCF-7 cells and in-silico analysis suggested their affinity towards hormone-dependent breast cancer. Compounds 4A1 to 4A3 exhibited the highest cytotoxicity against MCF-7 cells.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Oncology
Behnaz Lahooti, Sagun Poudel, Constantinos M. Mikelis, George Mattheolabakis
Summary: Angiogenesis is crucial for tumor growth and metastasis, with miRNAs playing a role in tumor progression. Current anti-angiogenic approaches provide clinical benefit but come with significant side effects.
FRONTIERS IN ONCOLOGY
(2021)
