Category: 438630-64-9

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 1H-Pyrazole-4-sulfonyl chloride, is researched, Molecular C3H3ClN2O2S, CAS is 438630-64-9, about Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.Related Products of 438630-64-9.

One of the challenges for targeting B-RafV600E with small mol. inhibitors had been achieving adequate selectivity over the wild-type protein B-RafWT, as inhibition of the latter has been associated with hyperplasia in normal tissues. Recent studies suggest that B-Raf inhibitors inducing the ‘DFG-in/αC-helix-out’ conformation (Type IIB) likely will exhibit improved selectivity for B-RafV600E. To explore this hypothesis, we transformed Type IIA inhibitor (1) into a series of Type IIB inhibitors (sulfonamides and sulfamides 4-6) and examined the SAR. Three selectivity indexes were introduced to facilitate the analyses: the B-RafV600E/B-RafWT biochem. (bS), cellular (cS) selectivity, and the phospho-ERK activation (pA). Our data indicates that α-branched sulfonamides and sulfamides show higher selectivities than the linear derivatives We rationalized this finding based on anal. of structural information from the literature and provided evidence for a monomeric B-Raf-inhibitor complex previously hypothesized to be responsible for the desired B-RafV600E selectivity.

Here is a brief introduction to this compound(438630-64-9)Related Products of 438630-64-9, if you want to know about other compounds related to this compound(438630-64-9), you can read my other articles.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling》. Authors are Liu, Longbin; Lee, Matthew R.; Kim, Joseph L.; Whittington, Douglas A.; Bregman, Howard; Hua, Zihao; Lewis, Richard T.; Martin, Matthew W.; Nishimura, Nobuko; Potashman, Michele; Yang, Kevin; Yi, Shuyan; Vaida, Karina R.; Epstein, Linda F.; Babij, Carol; Fernando, Manory; Carnahan, Josette; Norman, Mark H..The article about the compound:1H-Pyrazole-4-sulfonyl chloridecas:438630-64-9,SMILESS:ClS(=O)(=O)C1=CNN=C1).Name: 1H-Pyrazole-4-sulfonyl chloride. Through the article, more information about this compound (cas:438630-64-9) is conveyed.

One of the challenges for targeting B-RafV600E with small mol. inhibitors had been achieving adequate selectivity over the wild-type protein B-RafWT, as inhibition of the latter has been associated with hyperplasia in normal tissues. Recent studies suggest that B-Raf inhibitors inducing the ‘DFG-in/αC-helix-out’ conformation (Type IIB) likely will exhibit improved selectivity for B-RafV600E. To explore this hypothesis, we transformed Type IIA inhibitor (1) into a series of Type IIB inhibitors (sulfonamides and sulfamides 4-6) and examined the SAR. Three selectivity indexes were introduced to facilitate the analyses: the B-RafV600E/B-RafWT biochem. (bS), cellular (cS) selectivity, and the phospho-ERK activation (pA). Our data indicates that α-branched sulfonamides and sulfamides show higher selectivities than the linear derivatives We rationalized this finding based on anal. of structural information from the literature and provided evidence for a monomeric B-Raf-inhibitor complex previously hypothesized to be responsible for the desired B-RafV600E selectivity.

Here is a brief introduction to this compound(438630-64-9)Name: 1H-Pyrazole-4-sulfonyl chloride, if you want to know about other compounds related to this compound(438630-64-9), you can read my other articles.

Reference:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts