149507-31-3Relevant academic research and scientific papers
Substituted diarylurea derivative as well as preparation method and application thereof
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Paragraph 0089-0092; 0157-0159, (2021/08/19)
The invention relates to a substituted diarylurea derivative as well as preparation and application thereof. Specifically, the invention discloses a compound with a formula (I) or an optical isomer, a cis-trans-isomer or a pharmaceutically acceptable salt thereof, and a preparation method thereof, wherein the definition of each substituent group in the general formula is described in the specification and claims. The invention further discloses a composition containing the compound and application of the composition. The compound disclosed by the invention has excellent anti-cancer activity on HepG2 liver cancer cells, MGC 803 gastric cancer cells, MCF 7 breast cancer cells and the like, and has a good inhibition effect on the growth of human umbilical vein endothelial cells (HUVEC).
ARYL SULFONAMIDES AS SMALL MOLECULE STAT3 INHIBITORS
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, (2021/01/29)
The present disclosure provides pharmaceutical compositions comprising aryl sulfonamide Stat3 small molecule inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use for treating cancer.
Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide
Kankanala, Jayakanth,Ribeiro, Carlos J. A.,Kiselev, Evgeny,Ravji, Azhar,Williams, Jessica,Xie, Jiashu,Aihara, Hideki,Pommier, Yves,Wang, Zhengqiang
supporting information, p. 4669 - 4682 (2019/05/17)
Topoisomerase II (TOP2) poisons as anticancer drugs work by trapping TOP2 cleavage complexes (TOP2cc) to generate DNA damage. Repair of such damage by tyrosyl DNA phosphodiesterase 2 (TDP2) could render cancer cells resistant to TOP2 poisons. Inhibiting TDP2, thus, represents an attractive mechanism-based chemosensitization approach. Currently known TDP2 inhibitors lack cellular potency and/or permeability. We report herein two novel subtypes of the deazaflavin TDP2 inhibitor core. By introducing an additional phenyl ring to the N-10 phenyl ring (subtype 11) or to the N-3 site of the deazaflavin scaffold (subtype 12), we have generated novel analogues with considerably improved biochemical potency and/or permeability. Importantly, many analogues of both subtypes, particularly compounds 11a, 11e, 12a, 12b, and 12h, exhibited much stronger cancer cell sensitizing effect than the best previous analogue 4a toward the treatment with etoposide, suggesting that these analogues could serve as effective cellular probes.
BUILDING BLOCKS FOR DNA BINDING AGENTS
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Page/Page column 29, (2008/06/13)
The invention provides an alkylator that is an analog of a compound based on 5-oxo-1a,2,3,5-tetrahydro-1H-3-aza-cyclopropa[c]indene-7-carboxylic acid, 9a-chloromethyl-4-oxo-2,4,9,9a-tetrahydro-1H-2-aza-cyclopropa[1,5]cyclopenta[1,2-a]naphthalene-7-carboxylic acid, or 4-oxo-1,2,4,5,8,8a-hexahydrocyclopropa[c]pyrrolo[3,2-e]indole-6-carboxylic acid and conjugates thereof.
The Lindlar Catalyst Revitalized: A Highly Chemoselective Method for the Direct Conversion of Azides to N-(tert-Butoxycarbonyl)amines
Reddy, P. Ganapati,Pratap, T. Verabhadra,Kumar, G. D. Kishore,Mohanty, Subhendu K.,Baskaran, Sundarababu
, p. 3740 - 3744 (2007/10/03)
An exceptionally chemoselective method for the direct conversion of azides to N-(tert-butoxycarbonyl)-protected amines under catalytic transfer-hydrogenation conditions, using the Lindlar catalyst, is reported. The extremely labile functional groups such as N-Cbz, benzyl ester are shown to be inert under the reaction conditions. The present method allows us to synthesize orthogonally protected (N-Cbz and N-Boc) 1,2-diamino systems, which will be immensely useful in organic synthesis.
