153912-60-8Relevant articles and documents
MCL-1 INHIBITOR MACROCYCLE COMPOUNDS FOR USE IN CLINICAL MANAGEMENT OF CONDITIONS CAUSED OR MEDIATED BY SENESCENT CELLS AND FOR TREATING CANCER
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Paragraph 0130, (2021/05/15)
This disclosure provides small-molecule compounds with Mcl-l inhibitory activity. Compounds provided in this disclosure promote apoptosis in senescent cells, particularly when combined with inhibitors of other Bcl family proteins. Compounds provided in this disclosure also promote apoptosis in cancer cells. Such compounds can be developed for treating senescent-related conditions, or as chemotherapeutic agents.
Pyrazole functionalized n-heterocyclic carbene ruthenium compound with anticancer activity and preparation method and application thereof
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, (2017/08/28)
The invention discloses a pyrazole functionalized n-heterocyclic carbene ruthenium compound with anticancer activity and a preparation method and application thereof. The pyrazole functionalized n-heterocyclic carbene ruthenium compound is prepared by using 5-methyl-1-hydrogen-pyrazole ethyl formate through alkylation, reduction, chlorination, salt formation and metal exchange reaction, and the general formula of the pyrazole functionalized n-heterocyclic carbene ruthenium compound is [LRu(p-cymene)Cl](X) (L=pyrazole functionalized n-heterocyclic carbene ligand, and X is anions). In the cytotoxicity test of breast cancer cells (Bcap-37), intestinal cancer cells (LoVo), gastric cancer cells (SCG7901) and cisplatin-resistant gastric cancer cells (SCG7901-R), the n-heterocyclic carbene ruthenium compound can effectively inhibit cancer cell division and reproduction. The n-heterocyclic carbene ruthenium compound is variable in structure, convenient to synthesize, stable in performance, environmentally friendly, capable of stably existing in air for a long time, and promising in application prospect of pharmaceutical industry and fine chemical engineering industry.
Synthesis and enzyme inhibitory activities of some new pyrazole-based heterocyclic compounds
Harit, Tariq,Malek, Fouad,Bali, Brahim El,Khan, Ajmal,Dalvandi, Kourosh,Marasini, Bishnu P.,Noreen, Shagufta,Malik, Rizwana,Choudhary, M. Iqbal,Khan, Sadia
, p. 2772 - 2778,7 (2020/08/24)
Three tridentate N,N-bis(3,5-dimethylpyrazol- 1-ylmethyl)-1-hydroxy-2- aminoethane (2), N,N-bis(3,5-dimethylpyrazol- 1-ylmethyl)-cyclohexylamine (3) and 2-[bis (1,5-dimethyl-1H-pyrazol-3-ylmethyl)amino]ethan-1-ol (4) are synthesized and spectroscopically characterized togetherwith 1-hydroxymethyl-3,5-dimethylpyrazole (1). These have been tested in inhibitory activities against various hyperactive enzymes like urease, β- glucuronidase, phosphodiesterase, α-chymotrypsin, acetylcholinesterase and butyrylcholinesterase. Compounds 1, 2 and 3 were found to be selective inhibitors of urease. Compound 4 was found to be selective inhibitor of butyrylcholinesterase. The nature of the junction between pyrazoles cycles determined the activities of these tripods. While the tripods are inactive towards urease or glucuronidase, they turn to be selective towards butyrylcholinesterase.