17076-72-1Relevant academic research and scientific papers
Development of an enzyme-linked immunosorbent assay for the pyrethroid insecticide cyhalothrin
Gao, Hongbin,Ling, Yun,Xu, Ting,Zhu, Weiwen,Jing, Hongyu,Sheng, Wei,Li, Qing,Li, Ji
, p. 5284 - 5291 (2006)
A competitive enzyme-linked immunosorbent assay (ELISA) was developed for detection of the pyrethroid insecticide cyhalothrin. Three haptens with an amine or propanoic acid terminus were synthesized and then conjugated with bovine serum albumin to give immunogens. Eight polyclonal antisera produced by rabbits were screened for titers and affinity using three different coating antigens. The antiserum CWB-C had the highest affinity with cyhalothrin and a low affinity with fenvalerate, fenpropathrin, deltamethrin, and fluvalinate. The half-maximum inhibition concentration for cyhalothrin was 37.2 μg/L, and the limit of detection was 4.7 μg/L. The recoveries of different concentrations of cyhalothrin (0.1-2500 μg/L) from fortified tap water, well water, and wastewater samples as determined with the ELISA were 81-114%.
Development of novel phenoxy-diketopiperazine-type plinabulin derivatives as potent antimicrotubule agents based on the co-crystal structure
Ding, Zhongpeng,Ma, Mingxu,Zhong, Changjiang,Wang, Shixiao,Fu, Zhangyu,Hou, Yingwei,Liu, Yuqian,Zhong, Lili,Chu, Yanyan,Li, Feng,Song, Cai,Wang, Yuxi,Yang, Jinliang,Li, Wenbao
, (2019/12/09)
The co-crystal structure of Compound 6b with tubulin was prepared and solved for indicating the binding mode and for further optimization. Based on the co-crystal structures of tubulin with plinabulin and Compound 6b, a total of 27 novel A/B/C-rings plinabulin derivatives were designed and synthesized. Their biological activities were evaluated against human lung cancer NCI-H460 cell line. The optimum phenoxy-diketopiperazine-type Compound 6o exhibited high potent cytotoxicity (IC50 = 4.0 nM) through SAR study of three series of derivatives, which was more potent than plinabulin (IC50 = 26.2 nM) and similar to Compound 6b (IC50 = 3.8 nM) against human lung cancer NCI-H460 cell line. Subsequently, the Compound 6o was evaluated against other four human cancer cell lines. Both tubulin polymerization assay and immunofluorescence assay showed that Compound 6o could inhibit microtubule polymerization efficiently. Furthermore, theoretical calculation of the physical properties and molecular docking were elucidated for these plinabulin derivatives. The binding mode of Compound 6o was similar to Compound 6b based on the result of molecular docking. The theoretical calculated LogPo/w and PCaco of Compound 6o were better than Compound 6b, which could enhance its cytostatic activity. Therefore, Compound 6o might be developed as a novel potent anti-microtubule agent.
Pyrimidine onium compound and application thereof
-
Paragraph 0198-0201, (2019/10/23)
The invention relates to a pyrimidine onium compound, nitride oxides, salt of the nitride oxides and a composition comprising the compound. The invention further relates to an application of the compound to plant pest control.
Trisubstituted-N-[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl] benzamides which inhibit P2X3 and P2X2/3 containing receptors
-
, (2008/06/13)
Compounds of formula (I) are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
