I found the field of Pharmacology & Pharmacy very interesting. Saw the article Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases published in 2019. SDS of cas: 98-17-9, Reprint Addresses Zhang, C (corresponding author), Univ Southern Calif, Loker Hydrocarbon Res Inst, Los Angeles, CA 90089 USA.; Zhang, C (corresponding author), Univ Southern Calif, Dept Chem, Los Angeles, CA 90089 USA.; Zhang, C (corresponding author), Univ Southern Calif, USG Norris Comprehens Canc Ctr, Los Angeles, CA 90089 USA.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol
One effective means to achieve inhibitor specificity for RAF kinases, an important family of cancer drug targets, has been to target the monomeric inactive state conformation of the kinase domain, which, unlike most other kinases, can accommodate sulfonamide-containing drugs such as vemurafenib and dabrafenib because of the presence of a unique pocket specific to inactive RAF kinases. We previously reported an alternate strategy whereby rigidification of a nonselective pyrazolo[3,4-d]pyrimidine-based inhibitor through ring closure afforded moderate but appreciable increases in selectivity for RAF kinases. Here, we show that a further application of the rigidification strategy to a different pyrazolopyrimidine-based scaffold dramatically improved selectivity for RAF kinases. Crystal structure analysis confirmed our inhibitor design hypothesis revealing that 21 engages an active-like state conformation of BRAF normally associated with poorly discriminating inhibitors. When screened against a panel of distinct cancer cell lines, the optimized inhibitor 21 primarily inhibited the proliferation of the expected BRAF(V600E)-harboring cell lines consistent with its kinome selectivity profile. These results suggest that rigidification could be a general and powerful strategy for enhancing inhibitor selectivity against protein kinases, which may open up therapeutic opportunities not afforded by other approaches.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles