FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3208614456> ?p ?o ?g. }

• W3208614456 endingPage "3455" @default.
• W3208614456 startingPage "3434" @default.
• W3208614456 abstract "Abstract Multicomponent reactions (MCRs) are a valuable tool for the sustainable synthesis of new molecules in a fast, effective and eco‐friendly manner, leading to the generation of structurally diverse libraries. Their application in synthetic organic chemistry and medicinal chemistry, in combination with privileged scaffolds, is gaining momentum in recent years. The Ugi reaction is one of the most widely used MCRs in medicinal chemistry, and it is even used for the synthesis of several active pharmaceutical ingredients. Isatin, known for its biological activities and synthetic versatility, has been vastly used in several MCRs, however it was rarely used in combination with the Ugi reaction. Herein we report the first library of isatin‐based Ugi 4 component reaction (U4CR) derivatives. Reaction optimization and scope were thoroughly explored, as well as mechanistic insights were obtained using DFT calculations. The resulting library was evaluated in what concerns its druglike properties, pharmacokinetic profile assessment in silico and antiproliferative activity in vitro , with several compounds bearing interesting druglike properties. Biological screening against six tumor cell lines, showed that the majority of the compounds display antiproliferative activity in the low and sub‐micromolar range, with the achievement of nanomolar activity (0.1 nM, 6.5 nM and 5.4 nM against HBL‐100, HeLa and WiDr, respectively) for the more active compound." @default.
• W3208614456 created "2021-11-08" @default.
• W3208614456 creator A5011123686 @default.
• W3208614456 creator A5018187132 @default.
• W3208614456 creator A5030045844 @default.
• W3208614456 creator A5035356691 @default.
• W3208614456 creator A5045499776 @default.
• W3208614456 creator A5061969973 @default.
• W3208614456 date "2021-11-12" @default.
• W3208614456 modified "2023-09-27" @default.
• W3208614456 title "Ugi Adducts of Isatin as Promising Antiproliferative Agents with Druglike Properties" @default.
• W3208614456 cites W1922397604 @default.
• W3208614456 cites W1963737263 @default.
• W3208614456 cites W1981737096 @default.
• W3208614456 cites W1983285232 @default.
• W3208614456 cites W1992173555 @default.
• W3208614456 cites W2000727431 @default.
• W3208614456 cites W2003076573 @default.
• W3208614456 cites W2011505858 @default.
• W3208614456 cites W2014767176 @default.
• W3208614456 cites W2015711605 @default.
• W3208614456 cites W2026392596 @default.
• W3208614456 cites W2034740737 @default.
• W3208614456 cites W2043509228 @default.
• W3208614456 cites W2044940020 @default.
• W3208614456 cites W2051597072 @default.
• W3208614456 cites W2052907531 @default.
• W3208614456 cites W2066273100 @default.
• W3208614456 cites W2070337064 @default.
• W3208614456 cites W2078327603 @default.
• W3208614456 cites W2079458939 @default.
• W3208614456 cites W2082903593 @default.
• W3208614456 cites W2098725758 @default.
• W3208614456 cites W2105649494 @default.
• W3208614456 cites W2109398918 @default.
• W3208614456 cites W2111677437 @default.
• W3208614456 cites W2121577438 @default.
• W3208614456 cites W2129636678 @default.
• W3208614456 cites W2143123320 @default.
• W3208614456 cites W2144295240 @default.
• W3208614456 cites W2150697053 @default.
• W3208614456 cites W2247581895 @default.
• W3208614456 cites W2334363452 @default.
• W3208614456 cites W2396930286 @default.
• W3208614456 cites W2508435359 @default.
• W3208614456 cites W2510846738 @default.
• W3208614456 cites W2511938130 @default.
• W3208614456 cites W2549836338 @default.
• W3208614456 cites W2593436234 @default.
• W3208614456 cites W2765225412 @default.
• W3208614456 cites W2774836366 @default.
• W3208614456 cites W2897658017 @default.
• W3208614456 cites W2908523772 @default.
• W3208614456 cites W2911515218 @default.
• W3208614456 cites W2953001136 @default.
• W3208614456 cites W2963875818 @default.
• W3208614456 cites W2964936130 @default.
• W3208614456 cites W2983083150 @default.
• W3208614456 cites W3000022095 @default.
• W3208614456 cites W3001455197 @default.
• W3208614456 cites W3012303473 @default.
• W3208614456 cites W3014094886 @default.
• W3208614456 cites W3023385275 @default.
• W3208614456 cites W3029842408 @default.
• W3208614456 cites W3042595256 @default.
• W3208614456 cites W3115936542 @default.
• W3208614456 cites W3127094332 @default.
• W3208614456 cites W3130309548 @default.
• W3208614456 cites W3132176385 @default.
• W3208614456 cites W4248107770 @default.
• W3208614456 doi "https://doi.org/10.1002/ajoc.202100684" @default.
• W3208614456 hasPublicationYear "2021" @default.
• W3208614456 type Work @default.
• W3208614456 sameAs 3208614456 @default.
• W3208614456 citedByCount "5" @default.
• W3208614456 countsByYear W32086144562022 @default.
• W3208614456 countsByYear W32086144562023 @default.
• W3208614456 crossrefType "journal-article" @default.
• W3208614456 hasAuthorship W3208614456A5011123686 @default.
• W3208614456 hasAuthorship W3208614456A5018187132 @default.
• W3208614456 hasAuthorship W3208614456A5030045844 @default.
• W3208614456 hasAuthorship W3208614456A5035356691 @default.
• W3208614456 hasAuthorship W3208614456A5045499776 @default.
• W3208614456 hasAuthorship W3208614456A5061969973 @default.
• W3208614456 hasConcept C104317684 @default.
• W3208614456 hasConcept C108204754 @default.
• W3208614456 hasConcept C161624437 @default.
• W3208614456 hasConcept C178790620 @default.
• W3208614456 hasConcept C185592680 @default.
• W3208614456 hasConcept C202751555 @default.
• W3208614456 hasConcept C21951064 @default.
• W3208614456 hasConcept C2775905019 @default.
• W3208614456 hasConcept C2777010268 @default.
• W3208614456 hasConcept C2777256644 @default.
• W3208614456 hasConcept C2777366897 @default.
• W3208614456 hasConcept C2779070456 @default.
• W3208614456 hasConcept C55493867 @default.
• W3208614456 hasConcept C71240020 @default.

• next