1551-16-2Relevant articles and documents
Pyrrole Hemithioindigo Antimitotics with Near-Quantitative Bidirectional Photoswitching that Photocontrol Cellular Microtubule Dynamics with Single-Cell Precision**
Akhmanova, Anna,Heise, Constanze,Meiring, Joyce C. M.,Pettersson, Linda N.,Sailer, Alexander,Thorn-Seshold, Julia,Thorn-Seshold, Oliver
, p. 23695 - 23704 (2021/10/05)
We report the first cellular application of the emerging near-quantitative photoswitch pyrrole hemithioindigo, by rationally designing photopharmaceutical PHTub inhibitors of the cytoskeletal protein tubulin. PHTubs allow simultaneous visible-light imaging and photoswitching in live cells, delivering cell-precise photomodulation of microtubule dynamics, and photocontrol over cell cycle progression and cell death. This is the first acute use of a hemithioindigo photopharmaceutical for high-spatiotemporal-resolution biological control in live cells. It additionally demonstrates the utility of near-quantitative photoswitches, by enabling a dark-active design to overcome residual background activity during cellular photopatterning. This work opens up new horizons for high-precision microtubule research using PHTubs and shows the cellular applicability of pyrrole hemithioindigo as a valuable scaffold for photocontrol of a range of other biological targets.
Synthesis process method of 3-substituted-1H-pyrrole
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Paragraph 0158-0160; 0167-0168; 0171, (2020/05/30)
The invention provides a synthetic process method of a 3-substituted-1H-pyrrole compound. The process method comprises the following steps: by taking diethylamine hydrochloride and glycine ethyl esterhydrochloride as initial raw materials, respectively carrying out Mannich reaction and sulfamide reaction, and carrying out cyclization reaction, dehydration thinning reaction, aromatization reactionand hydrolysis decarboxylation reaction to obtain a 3-substituted-1H-pyrrole compound. According to the synthesis process method of the 3-substituted-1H-pyrrole compound, the whole synthesis route isgood in step repeatability, mild in operation condition and high in safety, and large-scale production and industrial popularization are facilitated; post-treatment energy consumption is low, a largeamount of toxic wastewater is not generated, no pollution is caused to the environment, the production safety level and the production cost are reduced, application of green and environment-friendlyindustrial production is facilitated, and wide application prospects are achieved.
Synthesis of 2,2′-bipyrrole-5-carboxaldehydes and their application in the synthesis of B-ring functionalized prodiginines and tambjamines
Kancharla, Papireddy,Reynolds, Kevin A.
, p. 8375 - 8385 (2013/09/02)
Facile, versatile, and cost-effective synthetic routes for the preparation of a range of new 3-alkyl-, 4-alkyl-, 3,4-dialkyl-, and 3-halo-4-alkyl-2, 2′-bipyrrole-5-carboxaldehydes have been developed. These 2,2′-bipyrrole-5-carboxaldehydes offer interesting potential as building blocks for making bioactive natural and unnatural products, as demonstrated by the synthesis of B-ring functionalized prodiginines (PGs) and tambjamines.