66962-18-3Relevant academic research and scientific papers
Synthesis and antibacterial activity of substituted thiosemicarbazides and of 1,3,4-thiadiazole or 1,2,4-triazole derivatives
Spalinska, Katarzyna,Foks, Henryk,Kedzia, Anna,Wierzbowska, Marta,Kwapisz, Ewa,Gebska, Alina,Ziolkowska-Klinkosz, Marta
, p. 609 - 625 (2006)
The synthesized series of new thiosemicarbazide derivatives (1, 6-10) in reactions with carbon disulphide produced, according to the reaction conditions, the dithioacids (4, 30) or the 5-substituted l,3,4-thiadiazolo-2-thiol derivatives (2, 27). The dithi
Dithiocarbamation of spiro-aziridine oxindoles: a facile access to C3-functionalised 3-thiooxindoles as apoptosis inducing agents
Bhandari, Sonal,Godugu, Chandraiah,Laxmikeshav, Kritika,Panda, Biswajit,Sakla, Akash P.,Shankaraiah, Nagula,Soni, Jay Prakash
, p. 10622 - 10634 (2021/12/27)
Herein, we report the first dithiocarbamation of spiro-aziridine oxindoles involving regiospecific ring-opening by usingin situgenerated nucleophilic dithiocarbamates as an instant source of sulfur. This approach afforded C3-functionalised-3-thiooxindoles in good to excellent yields with a wide substrate scope under catalyst-free and mild reaction conditions. These compounds were screened for their anticancer activity against a panel of human cancer cell lines, wherein compound3uexhibited significant cytotoxic activity against human lung cancer cells with an IC50value of 4.31 ± 1.88 μM. Phase contrast microscopy as well as different staining assays such as acridine orange/ethidium bromide (AO/EB), DAPI and DCFDA demonstrated the induction of apoptosis in A549 lung cancer cells after treatment with compound3u. In addition, the clonogenic assay and migration assay demonstrated the ability of compound3uto inhibit colony formation and cell migration, respectively, in A549 cells in a dose-dependent manner.
Synthesis, antifungal activities and molecular docking studies of novel 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl dithiocarbamates
Zou, Yan,Yu, Shichong,Li, Renwu,Zhao, Qingjie,Li, Xiang,Wu, Maocheng,Huang, Ting,Chai, Xiaoxun,Hu, Honggang,Wu, Qiuye
, p. 366 - 374 (2014/02/14)
A series of 2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl) propyl dithiocarbamates as new analogs of fluconazole were synthesized and their antifungal activities were evaluated. Among these compounds, 2a-f and 3a-q exhibited higher activities than fluconazole against nearly all fungi tested except Aspergillus fumigatus. Noticeably, the in vitro biological activities of 2b, 3a, 3c, 3h-k, and 3o-q against Candida species were much better than those of fluconazole and ketoconazole. Also, 2a-d, 3a-d, 3e-f, 3h-k, 3p and 3q showed higher activities against A. fumi than fluconazole. Computational docking experiments indicated that the inhibition of CYP51 involved a coordination bond with iron of the heme group, the hydrophilic H-bonding region, the hydrophobic region, and the narrow hydrophobic cleft.
Synthesis and cytotoxicity screening of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones
Cao, Sheng-Li,Guo, Yan-Wen,Wang, Xian-Bo,Zhang, Mei,Feng, Yu-Ping,Jiang, Yu-Yang,Wang, Yue,Gao, Qian,Ren, Jian
experimental part, p. 182 - 189 (2009/05/26)
A new series of piperazine-1-carbodithioate derivatives of 2-substituted quinazolin-4(3H)-ones were synthesized via a five-steps procedure starting from 2-amino-5-methylbenzoic acid. The cytotoxicity of the resulting compounds against A-549 (human lung ca
