An Efficient Protocol for the Synthesis of 1, 5‐ disubstituted Tetrazole Derivatives via a TMS‐N3 Based Ugi Reaction and their Anti‐cancer Activity,ChemistrySelect

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An Efficient Protocol for the Synthesis of 1, 5‐ disubstituted Tetrazole Derivatives via a TMS‐N3 Based Ugi Reaction and their Anti‐cancer Activity
ChemistrySelect ( IF 1.9 ) Pub Date : 2018-11-06 , DOI: 10.1002/slct.201802638
Jyoti N. Gohel ₁ , Kaushikkumar S. Lunagariya ₁ , Khushal M. Kapadiya ₂ , Ranjan C. Khunt ₁

Affiliation

In current research scenario, an efficient synthesis has been developed for novel tetrazole scaffolds by single step multicomponent reaction. One of the most promising pathways is Ugi multi‐component process for the coupling of four different components in a single reaction step and isolate lead molecule which may serve better life to the society. The syntheses of tetrazoles were undertaken by the Ugi‐Multi Component approach with the condensation of aromatic aldehyde containing active pharmacophore, various aryl amines, isocyanide (cyclohexyl isocyanide) and TMS‐N₃ under catalyst free reaction condition at room temperature. The structural conformation were carried out by most acceptable spectroscopic technique i.e. MS, IR, NMR and single crystal study (XRD) and potency of compounds (4a to 4h) were checked at NIH (National Institute of Health) use 60 different cell‐lines with respect to nine cancer panels among which compounds 4a and 4b have been found to be more potent against different cell lines.

中文翻译：

通过基于TMS-N3的Ugi反应合成1，5-二取代的四唑衍生物的有效方案及其抗癌活性

在当前的研究场景中，已经通过单步多组分反应开发了用于新型四唑支架的有效合成方法。最有前途的途径之一是Ugi多组分过程，可在单个反应步骤中偶联四种不同的组分，并分离出可能为社会带来更好生活的铅分子。四唑的合成是通过Ugi-Multi Component方法进行的，在室温下，在无催化剂的条件下，将含芳香醛的活性药效团，各种芳基胺，异氰酸酯（环己基异氰化物）和TMS-N ₃缩合。结构构象，通过最上可接受的光谱技术进行，即。MS，IR，NMR和单晶研究（XRD）以及化合物的功效在NIH（美国国立卫生研究院）检查（4a至4h）时，使用了60种不同的细胞系，涉及9种癌症研究小组，其中发现化合物4a和4b对不同的细胞系更有效。

更新日期：2018-11-06

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