- Spiro indolone compound as well as, preparation, method and pharmaceutical composition and application thereof
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Spiro indolone compounds, a preparing method, a medicine composition and uses of the compounds are disclosed. In particular, the invention provide spiro indolone compounds shown as a formula I or II, a preparing method of the spiro indolone compounds and
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Paragraph 0158-0161
(2020/01/11)
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- Synthesis and biological evaluation of 5′-phenyl-3′H-spiro- [indoline-3,2′-[1,3,4]oxadiazol]-2-one analogs
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A series of 5′-phenyl-3′H-spiro[indoline-3,2′-[1,3,4] thiadiazol]-2-one analogs were synthesized and their Bcl-2 protein inhibitory activities were studied. The lead compound was originally identified using a fluorescence polarization-based competitive binding assay. Among the 10 compounds investigated, 1k showed good binding affinities to Bcl-xL and Mcl-1, with inhibition constants of 8.9 μmol/L and 3.4 μmol/L, respectively. While compound 1c achieved tight binding affinities to Bcl-xL (Ki = 0.16 μmol/L), has the potential to be a new lead compound.
- Liu, Hua-Quan,Wang, De-Cai,Wu, Fei,Tang, Wei,Ouyang, Ping-Kai
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p. 929 - 933
(2013/09/24)
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- Thiadiazole compounds and methods of use thereof
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The present invention relates to Thiadiazole Compounds; compositions comprising an effective dose of a Thiadiazole Compound; and methods treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, cancer, r
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Page/Page column 27
(2008/12/05)
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- 5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2)
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5′-Phenyl-3′H-spiro[indoline-3,2′-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared via commercially available starting materials. Selected compounds 23, 33-35 show sub-micromolar ADAMTS-5 potency and strong SAR trends with selectivity over the related metalloproteases ADAMTS-4 (Aggrecanase-1), MMP12, and MMP13. This series of compounds represents progress toward a selective ADAMTS-5 inhibitor as a disease modifying osteoarthritis drug.
- Bursavich, Matthew G.,Gilbert, Adam M.,Lombardi, Sabrina,Georgiadis, Katy E.,Reifenberg, Erica,Flannery, Carl R.,Morris, Elisabeth A.
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p. 5630 - 5633
(2008/03/14)
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- SEMICARBAZONES AND THIOSEMICARBAZONES OF THE HETEROCYCLIC SERIES. XLIV. CYCLIZATION OF ISATIN AND 1-ACETYLISATIN 3-THIOBENZOYLHYDRAZONES
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Isatin 3-thiobenzoylhydrazone undergoes cyclization with the addition of the sulfur atom to the C3 atom and closure of the thiadiazole ring.In contrast, 3-thioaroylhydrazones of 1-acetylisatin undergo cyclization with participation of C2 and close the thiadiazine ring with the formation of derivatives of the new heterocyclic system thiadiazinoindole.
- Tomchin, A.B.
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p. 504 - 510
(2007/10/02)
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