1228284-98-7Relevant academic research and scientific papers
Small molecules inhibit STAT3 activation, autophagy, and cancer cell anchorage-independent growth
Zhou, Donghui,Springer, Maya Z.,Xu, David,Liu, Degang,Hudmon, Andy,Macleod, Kay F.,Meroueh, Samy O.
, p. 2995 - 3005 (2017/05/29)
Triple-negative breast cancers (TNBCs) lack the signature targets of other breast tumors, such as HER2, estrogen receptor, and progesterone receptor. These aggressive basal-like tumors are driven by a complex array of signaling pathways that are activated by multiple driver mutations. Here we report the discovery of 6 (KIN-281), a small molecule that inhibits multiple kinases including maternal leucine zipper kinase (MELK) and the non-receptor tyrosine kinase bone marrow X-linked (BMX) with single-digit micromolar IC50s. Several derivatives of 6 were synthesized to gain insight into the binding mode of the compound to the ATP binding pocket. Compound 6 was tested for its effect on anchorage-dependent and independent growth of MDA-MB-231 and MDA-MB-468 breast cancer cells. The effect of 6 on BMX prompted us to evaluate its effect on STAT3 phosphorylation and DNA binding. The compound's inhibition of cell growth led to measurements of survivin, Bcl-XL, p21WAF1/CIP1, and cyclin A2 levels. Finally, LC3B-II levels were quantified following treatment of cells with 6 to determine whether the compound affected autophagy, a process that is known to be activated by STAT3. Compound 6 provides a starting point for the development of small molecules with polypharmacology that can suppress TNBC growth and metastasis.
NOVEL PYRAZOLE-4-N-ALKOXYCARBOXAMIDES AS MICROBIOCIDES
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Page/Page column 20, (2011/10/10)
Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.
NOVEL MICROBIOCIDES
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Page/Page column 44-45, (2010/06/20)
Compounds of formula (I) in which the substituents are as defined in claim 1,are suitable for use as microbiocides.
Practical and chemoselective reduction of acyl chloride to alcohol by borohydride in aqueous dichloromethane
Rajan, Ramya,Badgujar, Sachin,Kaur, Kamaljit,Malpani, Yashwardhan,Kanjilal, Pranab R.
experimental part, p. 2897 - 2907 (2010/11/18)
A simple methodology for the reduction of acid chlorides to their corresponding alcohols has been developed. Various carboxylic acids were converted to alcohols in excellent yields using NaBH4-K2CO3 in a mixed solvent system of dichloromethane and water (1:1) in the presence of a phase-transfer catalyst at low temperature. The importance of the work is its simplicity, selectivity, excellent yield, and very short reaction time. This new reduction condition has proved to be an excellent chemoselective method for a range of acid chlorides in the presence of various functional groups.
NOVEL MICROBIOCIDES
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Page/Page column 24-25, (2009/12/02)
Compounds of formula I (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.
