Authors Chi, YH; Yeh, TK; Ke, YY; Lin, WH; Tsai, CH; Wang, WP; Chen, YT; Su, YC; Wang, PC; Chen, YF; Wu, ZW; Yeh, JY; Hung, MC; Wu, MH; Wang, JY; Chen, CP; Song, JS; Shih, C; Chen, CT; Chang, CP in AMER CHEMICAL SOC published article about SMALL-MOLECULE INHIBITORS; N-MYC; CANCER; DESIGN; IDENTIFICATION; TRANSITION; STRATEGY; PRODRUGS; INDUCE; TARGET in [Chi, Ya-Hui; Yeh, Teng-Kuang; Ke, Yi-Yu; Lin, Wen-Hsing; Tsai, Chia-Hua; Wang, Wan-Ping; Chen, Yen-Ting; Su, Yu-Chieh; Wang, Pei-Chen; Chen, Yan-Fu; Wu, Zhong-Wei; Yeh, Jen-Yu; Hung, Ming-Chun; Wu, Mine-Hsine; Wang, Jing-Ya; Chen, Ching-Ping; Song, Jen-Shin; Shih, Chuan; Chen, Chiung-Tong; Chang, Chun-Ping] Natl Hlth Res Inst, Inst Biotechnol & Pharmaceut Res, Zhunan 35053, Taiwan; [Chi, Ya-Hui] China Med Univ, Grad Inst Biomed Sci, Taichung 40402, Taiwan; [Chang, Chun-Ping] Chung Yuan Christian Univ, Dept Chem, Taoyuan 320314, Taiwan in 2021, Cited 45. Safety of 2,4-Dichlorobenzoic acid. The Name is 2,4-Dichlorobenzoic acid. Through research, I have a further understanding and discovery of 50-84-0
The A-type Aurora kinase is upregulated in many human cancers, and it stabilizes MYC-family oncoproteins, which have long been considered an undruggable target. Here, we describe the design and synthesis of a series of pyrimidine-based derivatives able to inhibit Aurora A kinase activity and reduce levels of cMYC and MYCN. Through structure-based drug design of a small molecule that induces the DFG-out conformation of Aurora A kinase, lead compound 13 was identified, which potently (IC50 < 200 nM) inhibited the proliferation of high-MYC expressing small-cell lung cancer (SCLC) cell lines. Pharmacokinetic optimization of 13 by prodrug strategies resulted in orally bioavailable 25, which demonstrated an 8-fold higher oral AUC (F = 62.3%). Pharmacodynamic studies of 25 showed it to effectively reduce cMYC protein levels, leading to >80% tumor regression of NCI-H446 SCLC xenograft tumors in mice. These results support the potential of 25 for the treatment of MYC-amplified cancers including SCLC.
Safety of 2,4-Dichlorobenzoic acid. About 2,4-Dichlorobenzoic acid, If you have any questions, you can contact Chi, YH; Yeh, TK; Ke, YY; Lin, WH; Tsai, CH; Wang, WP; Chen, YT; Su, YC; Wang, PC; Chen, YF; Wu, ZW; Yeh, JY; Hung, MC; Wu, MH; Wang, JY; Chen, CP; Song, JS; Shih, C; Chen, CT; Chang, CP or concate me.
Reference:
Chloride – Wikipedia,
,Chlorides – an overview | ScienceDirect Topics