94023-67-3Relevant academic research and scientific papers
Synthesis, Antileishmanial Activity and In Silico Studies of Aminoguanidine Hydrazones (AGH) and Thiosemicarbazones (TSC) Against Leishmania chagasi Amastigotes
Alexandre-Moreira, Magna S.,Aquino, Pedro G. V.,Bourguignon, Jean-Jacques,Bri-Card, Jacques,Freitas, Johnnatan D.,Meneghetti, Mario R.,Nascimento, Igor J. S.,Queiroz, Aline C.,Rodrigues, Klinger A. F.,Rodrigues, Raiza R. L.,Santos, Mariana S.,Schmitt, Martine,de Aquino, Thiago M.,Araújo, Morgana V.,Fran?a, Paulo H. B.,Rodrigues, érica E. E. S.,Santos-Júnior, Paulo F. S.,da Silva-Júnior, Edeildo F.,de Araújo-Júnior, Jo?o X.
, p. 151 - 169 (2022/02/05)
Background: Leishmaniasis is a worldwide health problem, highly endemic in developing countries. Among the four main clinical forms of the disease, visceral leishmaniasis is the most se-vere, fatal in 95% of cases. The undesired side-effects from first-li
Synthesis and biological activities of 2-amino-1-arylidenamino imidazoles as orally active anticancer agents
Li, Wen-Tai,Hwang, Der-Ren,Song, Jen-Shin,Chen, Ching-Ping,Chuu, Jiunn-Jye,Hu, Chih-Bo,Lin, Heng-Liang,Huang, Chen-Lung,Huang, Chiung-Yi,Tseng, Huan-Yi,Lin, Chu-Chung,Chen, Tung-Wei,Lin, Chi-Hung,Wang, Hsin-Sheng,Shen, Chien-Chang,Chang, Chung-Ming,Chao, Yu-Sheng,Chen, Chiung-Tong
experimental part, p. 2409 - 2417 (2010/09/03)
2-Amino-l-arylidenaminoimidazoles, a novel class of orally (po) active microtubule-destabilizing anticancer agents, were synthesized. The compounds were designed from a hit compound identified in a drug discovery platform by using cancer cell-based high throughput screening assay. Selective synthesized compounds exerted cell cytotoxicity against human cancer cells. The underlying mechanisms for the anticancer activity were demonstrated as interacting with the tubulins and inhibiting microtubule assembly, leading to proliferation inhibition and apoptosis induction in the human tumor cells. Furthermore, two compounds showed in vivo anticancer activities in both po and intravenously (iv) administered routes and prolonged the life spans of murine leukemic P388 cells-inoculated mice. These new po active antimitotic anticancer agents are to be further examined in preclinical studies and developed for clinical uses.
