1325724-92-2Relevant articles and documents
Design, synthesis and biological evaluation of 1H-1,2,3-triazole-linked- 1H-dibenzo[b,h]xanthenes as inductors of ROS-mediated apoptosis in the breast cancer cell line MCF-7
Bortolot, Carolina S.,Forezi, Luana da S. M.,Marra, Roberta K. F.,Reis, Marcelo I. P.,e Sá, Bárbara V. F.,Filho, Ricardo I.,Ghasemishahrestani, Zeinab,Sola-Penna, Mauro,Zancan, Patricia,Ferreira, Vitor F.,da Silva, Fernando de C.
, p. 119 - 129 (2019/06/11)
Background: Low molecular weight 1,2,3-triazoles and naphthoquinones are endowed with various types of biological activity, such as against cancer, HIV and bacteria. However, in some cases, the conjugation of these two nuclei considerably increases their biological activities. Objective: In this work, we decided to study the synthesis and screening of bis-naphthoquinones and xanthenes tethered to 1,2,3-triazoles against cancer cell lines, specifically the human breast cancer cell line MCF-7. Results: Starting from lawsone and aryl-1H-1,2,3-triazole-4-carbaldehydes (10a-h) several new 7- (1-aryl-1H-1,2,3-triazol-4-yl)-6H-dibenzo[b,h]xanthene-5,6,8,13(7H)-tetraones (12a-h) and 3,3'- ((1-aryl-1H-1,2,3-triazol-4-yl)methylene)bis(2-hydroxynaphthalene-1,4-diones) 11a-h were synthesized and evaluated for their cytotoxic activities using the human breast cancer cell line MCF-7 and the non-tumor cell line MCF10A as control. We performed test of cell viability, cell proliferation, intracellular ATP content and cell cytometry to determine reactive oxygen species (ROS) formation. Conclusions: Based on these results, we found that compound 12a promotes ROS production, interfering with energy metabolism, cell viability and proliferation, and thus promoting whole cell damage.
Synthesis and biological evaluation of ursolic acid derivatives bearing triazole moieties as potential anti-Toxoplasma gondii agents
Luan, Tian,Jin, Chunmei,Jin, Chun-Mei,Quan, Zhe-Shan,Gong, Guo-Hua
, p. 761 - 772 (2019/03/23)
Ursolic acid (UA), a plant-derived compound, has many properties beneficial to health. In the present study, we synthesised three series of novel UA derivatives and evaluated their anti-Toxoplasma gondii activity both in vitro and in vivo. Most derivative
Design and synthesis of novel dehydroepiandrosterone analogues as potent antiproliferative agents
Huang, Xing,Shen, Qing-Kun,Zhang, Hong-Jian,Li, Jia-Li,Tian, Yu-Shun,Quan, Zhe-Shan
, (2018/09/12)
The aim of the present study was to determine the cytotoxic effects of a series of novel dehydroepiandrosterone derivatives containing triazole at the C16 position on human cancer cells. The cancer cells used in the present study were A549, Hel
Novel 1,2,3-triazole derivatives for use against mycobacterium tuberculosis H37Rv (ATCC 27294) strain
Boechat, Nubia,Ferreira, Vitor F.,Ferreira, Sabrina B.,Ferreira, Maria De Lourdes G.,Da Silva, Fernando De C.,Bastos, Monica M.,Costa, Marilia Dos S.,Louren?o, Maria Cristina S.,Pinto, Angelo C.,Krettli, Antoniana U.,Aguiar, Anna Caroline,Teixeira, Brunno M.,Da Silva, Nathalia V.,Martins, Priscila R. C.,Bezerra, Flavio Augusto F. M.,Camilo, Ane Louise S.,Da Silva, Gerson P.,Costa, Carolina C. P.
, p. 5988 - 5999 (2011/10/09)
The purpose of this study was to prepare various 4-substituted N-phenyl-1,2,3-triazole derivatives using click chemistry. The derivatives were screened in vitro for antimicrobial activity against Mycobacterium tuberculosis strain H37Rv (ATCC 27294) using
