59960-75-7Relevant academic research and scientific papers
Benzothiazole carbamates and amides as antiproliferative species
Videnovi?, Milica,Mojsin, Marija,Stevanovi?, Milena,Opsenica, Igor,Srdi?-Raji?, Tatjana,?olaja, Bogdan
supporting information, p. 1096 - 1114 (2018/10/16)
A series of new benzothiazole-based carbamates and amides were synthesized and their antiproliferative activity was determined. Derivatives with profound activity were identified and further investigated for their possible mechanism of action. It was found that these compounds induce specific apoptosis, G2/M cell cycle arrest and decrease ROS level in MCF-7 human breast cancer cell line. Moreover, submicromolar antiproliferative activity of examined carbamates against NT2/D1 testicular embryonal carcinoma was shown. The most potent derivatives strongly inhibited NT2/D1 cell migration and invasiveness.
Synthesis and methemoglobinemia-inducing properties of analogues of para-aminopropiophenone designed as humane rodenticides
Rennison, David,Conole, Daniel,Tingle, Malcolm D.,Yang, Junpeng,Eason, Charles T.,Brimble, Margaret A.
, p. 6629 - 6635 (2014/01/06)
A number of structural analogues of the known toxicant para- aminopropiophenone (PAPP) have been prepared and evaluated for their capacity to induce methemoglobinemia - with a view to their possible application as humane pest control agents. It was found that an optimal lipophilicity for the formation of methemoglobin (metHb) in vitro existed for alkyl analogues of PAPP (aminophenones 1-20; compound 6 metHb% = 74.1 ± 2). Besides lipophilicity, this structural sub-class suggested there were certain structural requirements for activity, with both branched (10-16) and cyclic (17-20) alkyl analogues exhibiting inferior in vitro metHb induction. Of the four candidates (compounds 4, 6, 13 and 23) evaluated in vivo, 4 exhibited the greatest toxicity. In parallel, aminophenone bioisosteres, including oximes 30-32, sulfoxide 33, sulfone 34 and sulfonamides 35-36, were found to be inferior metHb inducers to lead ketone 4. Closer examination of Hammett substituent constants suggests that a particular combination of the field and resonance parameters may be significant with respect to the redox mechanisms behind PAPPs metHb toxicity.
Synthesis and in vitro antifungal activity of 4-substituted phenylguanidinium salts
Braunerova, Gabriela,Buchta, Vladimir,Silva, Luis,Kunes, Jiri,Palat Jr., Karel
, p. 443 - 450 (2007/10/03)
A series of 4-substituted phenylguanidinium derivatives was synthesized and its antimicrobial activity was evaluated in vitro against eight potentially pathogenic strains of fungi.
