Finding the rules for successful drug optimisation Drug Discovery Today Volume 19, Issue 5 , May 2014, Pages 680–687 口服药先导化合物选择的基本标准, 包括活性、物化性质、药代性质与安全性标准。
http://cen.acs.org/articles/92/web/2014/05/Tug-War-Over-Promising-Cancer.html Tug Of War Over Promising Cancer Drug Candidate TIC10 or ONC201 是一种高效的抗癌分子,通过激发肿瘤坏死因子相关凋亡诱导配体的基因表达(tumor necrosis factor related apoptosis?inducing ligand TRAIL,TRAIL其受体结 ...
Synthesis, Structure − Activity Relationships, and in Vivo E ffi cacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5 ‑ Chloro ‑ N 2 ‑ (2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl) ‑ N 4 (2-(isopropylsulfonyl)pheny ...
Pyrazolopyridine inhibitors of B-RafV600E. Part 3: An increase in aqueous solubility via the disruption of crystal packing S. Wenglowsky et al. / Bioorg. Med. Chem. Lett. 22 (2012) 912 – 915 吡唑嘧啶类化合物 1,2 的缺点在于溶解性 ...
Pyrazolopyridine Inhibitors of B-Raf V600E Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors ACS Med. Chem. Lett. 2011, 2, 342 – 347 在 PLX4032 ( Vemurafenib ...