Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors was written by Sun, Ying;Shan, Yuanyuan;Li, Chuansheng;Si, Ru;Pan, Xiaoyan;Wang, Binghe;Zhang, Jie. And the article was included in European Journal of Medicinal Chemistry in 2017.Safety of 2,4-Dichlorophenylisothiocyanate This article mentions the following:
VEGFR-2, TIE-2, and EphB4 are essential for both angiogenesis and tumorigenesis. Herein, the authors designed and prepared three classes of multi-target inhibitors based on the extensive sequence homol. along the kinase domain of angiogenic RTKs. Biol. evaluation indicated that these multi-target inhibitors exhibited considerable potential as novel anti-angiogenic and anticancer agents. Among them, a diaryl thiourea bearing 1H-indazole-3-amine (16a, N-[4-(3-amino-1H-indazol-4-yl)phenyl]-N’-[5-bromo-2-(trifluoromethoxy)phenyl]thiourea) displayed the most potent RTK inhibition and excellent selectivity. It also showed inhibition on viability of human umbilical vein endothelial cells and anti-proliferation against a broad spectrum of cancer cells. Therefore, 1H-indazole-3-amine could serve as a promising hinge binding group for multi-target inhibitors of VEGFR-2, Tie-2, and EphB4. In the experiment, the researchers used many compounds, for example, 2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1Safety of 2,4-Dichlorophenylisothiocyanate).
2,4-Dichlorophenylisothiocyanate (cas: 6590-96-1) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Safety of 2,4-Dichlorophenylisothiocyanate
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics