Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.
Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.
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DOI：
10.1021/cc100128w
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发表时间：
2010-11-08
影响因子：
--
通讯作者：
Zhang, Wei
中科院分区：
文献类型：
--
作者：
Dolle, Roland E.;Le Bourdonnec, Bertrand;Worm, Karin;Morales, Guillermo A.;Thomas, Craig J.;Zhang, Wei
这是高通量化学综合调查系列的第十三期。1 2009年报告的生物活性文库见表1-5，标题为蛋白酶、非蛋白水解酶、GPCR、非GPCR和溶瘤药/抗感染药。表6列出了分子探针。没有公开的生物活性的化合物集合在表7-10中在支架衍生化/无环合成、单环-、双环/螺环-和多环/大环合成的标题下描述。聚合物负载的试剂/清除剂/连接剂列于表11（非氟）和12（氟）中。从355篇文献中提取了370个文库和24个分子探针。2-172今年的18个小插曲包括（a）生物活性文库HDAC 1/HDAC 2抑制剂，134种H3拮抗剂，136种胰高血糖素受体拮抗剂，179种嘌呤能P2 Y12受体拮抗剂，221种热休克蛋白90（Hsp 90）抑制剂，41种选择性去甲肾上腺素再摄取抑制剂，182（d）通过3-组分反应的取代的胍289和取代的嘧啶的高通量化学方法学捕获-释放合成; 257（c）分子探针Ned-19340和DG-041; 338和（d）氟技术可置换的氟二氢吡喃322和异腈连接体，327 1，4-苯并二氮杂-2，5-二酮的氟合成，327哌嗪二酮稠合的三环化合物库，和天然产物间苯二酚内酯库的氟混合物合成。329 2009年出现的相关出版物和评论涉及微波辅助的N-杂环合成356和可转化的异腈，365点击化学，358动态组合化学，363硅官能化SynPhase灯笼的大规模制备，370激酶抑制剂，357热休克蛋白90抑制剂，376生物活性苯并稠合氮杂环，361文库自动化和分析，360，368文库设计，375基于NMR的筛选，377，378片段文库和片段跳跃，366，367，369 Ellman文库的回顾，374固相树脂规格，359用于监测配体-受体结合事件的微电极阵列，364用于小分子进化的微升级DNA反应器，362 DNA编码库，379和荧光化学和分离。380-383在一个由三部分组成的系列中，Scott和同事提议激励全球高通量化学社区在“分布式药物发现”的背景下分享技术，资源和化合物，以找到治疗发展中国家疾病的方法。371-373
This is the thirteenth installment of the comprehensive survey series in high-throughput chemistry. 1 Biologically active libraries reported in 2009 are captured in Tables 1-5 under the headings of proteases, nonproteolytic enzymes, GPCRs, nonGPCRs, and oncolytics/antiinfectives. Table 6 lists molecular probes. Compound collections without disclosed biological activity are delineated in Tables 7-10 under the headings of scaffold derivatization/acyclic synthesis, monocyclic-, bicyclic/spirocyclic-, and polycyclic/macrocyclic synthesis. Polymer-supported reagents/scavengers/linkers are presented in Tables 11 (nonfluorous) and 12 (fluorous). There are 370 libraries and 24 molecular probes extracted from 355 literature citations. 2-172 This year’s 18 vignettes include (a) biologically active libraries HDAC1/HDAC2 inhibitors, 134 H3 antagonists, 136 glucagon receptor antagonists, 179 purinergic P2Y12 receptor antagonists, 221 heat shock protein 90 (Hsp90) inhibitors, 41 selective norepinephrine reuptake inhibitors, 73 allosteric modulators of mGluR4287 and mGluR571 Bcl-2 inhibitors via DOS library; 182 (d) high-throughput chemical methodology catch-and-release synthesis of substituted guanidines289 and substituted pyrimidines via a 3-component reaction; 257 (c) molecular probes Ned-19340 and DG-041; 338 and (d) fluorous technology displaceable fluorous dihydropyran322 and isonitrile linkers, 327 fluorous synthesis of 1, 4-benzodiazepine-2, 5-dione, 327 piperazinedion-fused tricyclic328 compound libraries, and a fluorous mixture synthesis of natural product resorcyclic acid lactone library. 329 Related publications and reviews appeared in 2009 on microwave-assisted of N-heterocyclic synthesis356 and convertible isonitriles, 365 click chemistry, 358 dynamic combinatorial chemistry, 363 large scale preparation of siliconfunctionalized SynPhase lanterns, 370 kinase inhibitors, 357 heat shock protein 90 inhibitors, 376 biologically active benzoannelated nitrogen heterocycles, 361 library automation and analysis, 360,368 library design, 375 NMR-based screening, 377,378 fragment libraries and fragment hopping, 366,367,369 review of Ellman’s libraries, 374 solid-phase resin specifications, 359 microelectrode arrays for monitoring ligand-receptor binding events, 364 yactoliter-scale DNA reactor for small molecule evolution, 362 DNA encoded libraries, 379 and fluorous chemistry and separations. 380-383 In a three-part series, Scott and co-workers proposed to galvanize the worldwide highthroughput chemistry community to share technology, resources, and compounds in the context of “Distributed Drug Discovery” to find treatments for diseases of the developing nations. 371-373
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影响因子：
3.2
作者：
Ali, Akbar;Ghosh, Animesh;Rana, Tariq M.
通讯作者：
Rana, Tariq M.
影响因子：
1.1
作者：
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影响因子：
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作者：
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Capretta, Alfredo
影响因子：
2.7
作者：
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通讯作者：
Wong, Melissa
影响因子：
3.5
作者：
Ayesa, Susana;Lindquist, Charlotta;Samuelsson, Bertil
通讯作者：
Samuelsson, Bertil