[EN] BENZAMIDE OR BENZAMINE COMPOUNDS USEFUL AS ANTICANCER AGENTS FOR THE TREATMENT OF HUMAN CANCERS<br/>[FR] COMPOSÉS BENZAMIDE OU BENZAMINE À UTILISER EN TANT QU'ANTICANCÉREUX POUR LE TRAITEMENT DE CANCERS HUMAINS
申请人:UNIV TEXAS
公开号:WO2017007634A1
公开(公告)日:2017-01-12
The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells.
Tetra-arylborate lipophilic anions as targeting groups
作者:Kishore K. Gaddale Devanna、Justyna M. Gawel、Tracy A. Prime、Filip Cvetko、Cristiane Benincá、Stuart T. Caldwell、Alexander Negoda、Andrew Harrison、Andrew M. James、Evgeny V. Pavlov、Michael P. Murphy、Richard C. Hartley
DOI:10.1039/d0cc07924c
日期:——
TPB lipophilic anions deliver cargoes to lysosomes and are excluded from mitochondria.
TPB疏水性阴离子将货物运送到溶酶体,并被排除在线粒体之外。
Photochemical C−H Amination of Ethers and Geminal Difunctionalization Reactions in One Pot
(nonaflyl, Nf) azide as the aminating reagent to give N-sulfonyl hemiaminals is reported. This enables unprecedented C(sp3 ) difunctionalization reactions, leading to diverse functionalized amino group containing compounds starting from simple ethers in onepot.
A new class of structurally rigid tricyclic chiralligands based on the hexahydropyrrolo[2,3‐b]indole skeleton has been rationally designed and the catalytic abilities in asymmetric catalysis have been shown in the enantioselective borane reduction of prochiralketones to afford the chiralalcohols in excellent yields and high enantioselectivities (up to 97% ee).
合理设计了基于六氢吡咯并[2,3- b ]吲哚骨架的一类新型结构刚性的三环手性配体,在不对称催化的前手性甲硼烷的对映选择性硼烷还原反应中显示出不对称催化的催化能力,从而得到了手性醇。优异的收率和高对映选择性(高达97%ee)。
Cobalt-Catalyzed Electrophilic Amination of Aryl- and Heteroarylzinc Pivalates with <i>N</i>
-Hydroxylamine Benzoates
作者:Yi-Hung Chen、Simon Graßl、Paul Knochel
DOI:10.1002/anie.201710931
日期:2018.1.22
Aryl‐ and heteroarylzincpivalates can be aminated with O‐benzoylhydroxylamines at 25 °C within 2–4 h in the presence of 2.5–5.0 % CoCl2⋅2 LiCl to furnish the corresponding tertiary arylated or heteroarylated amines in good yields. This electrophilicamination also provides access to diarylamines and aryl(heteroaryl)amines. A new tuberculosis drug candidate (Q203) was prepared in six steps and 56 %