55368-83-7Relevant academic research and scientific papers
Microwave-assisted synthesis of new 2-aryl and 2-alkylimidazolones and evaluation of their in vitro anticancer activity and their in vivo toxicity on zebrafish embryos
Bou Zeid, Samar,Hamade, Aline,Najjar, Fadia,Carreaux, Francois,Eid, Samar
, p. 2549 - 2560 (2021/02/05)
Herein we describe the synthesis of five new 2-aryl and 2-alkylimidazolone derivatives via an effective one-pot synthetic strategy assisted by microwave irradiations which allowed us to access the desired product in a reduced time reaction compared to the
DNA-Encoded Libraries: Hydrazide as a Pluripotent Precursor for On-DNA Synthesis of Various Azole Derivatives
Ma, Fei,Li, Jie,Zhang, Shuning,Gu, Yuang,Tan, Tingting,Chen, Wanting,Wang, Shuyue,Ma, Peixiang,Xu, Hongtao,Yang, Guang,Lerner, Richard A.
supporting information, p. 8214 - 8220 (2021/05/03)
DNA-encoded combinatorial chemical library (DEL) technology, an approach that combines the power of genetics and chemistry, has emerged as an invaluable tool in drug discovery. Skeletal diversity plays a fundamental importance in DEL applications, and relies heavily on novel DNA-compatible chemical reactions. We report herein a phylogenic chemical transformation strategy using DNA-conjugated benzoyl hydrazine as a common versatile precursor in azole chemical expansion of DELs. DNA-compatible reactions deriving from the common benzoyl hydrazine precursor showed excellent functional group tolerance with exceptional efficiency in the synthesis of various azoles, including oxadiazoles, thiadiazoles, and triazoles, under mild reaction conditions. The phylogenic chemical transformation strategy provides DELs a facile way to expand into various unique chemical spaces with privileged scaffolds and pharmacophores.
Synthesis method of 1-alkyl-3, 5-aryl substituted 1, 2, 4 triazole compound
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Paragraph 0071; 0074-0076; 0101; 0104-0106, (2021/03/13)
The invention discloses a preparation method of a 1-alkyl-3, 5-aryl substituted 1, 2, 4 triazole compound, which comprises the following steps: reacting a cyano group-containing compound 1 with acetylchloride at 10-40 DEG C to convert the cyano group into an imino group, thereby generating a compound 2; carrying out amidation reaction on the compound 2 and a formyl chloride group-containing compound 3 at the temperature of 0 DEG C to 60 DEG C to generate a compound 4; subjecting the compound 4 and an alkyl hydrazine compound 5 to an oxidation ring closing reaction at the temperature of 0 DEGC to 60 DEG C, and generating a 1-alkyl-3, 5-aryl substituted 1, 2, 4-triazole compound 6; and carrying out hydrolysis reaction on ester in the compound 6 at the temperature of 25 DEG C to 80 DEG C togenerate carboxyl, so as to obtain the 1-alkyl-3, 5-aryl substituted 1, 2, 4 triazole compound 7 with halogen and carboxyl on two different aromatic rings respectively. The method has the advantagesof wide raw material application range, mild conditions, good reaction selectivity, no introduction of metal residues, easiness in operation and the like.
SUBSTITUTED PYRAZOLOPYRIMIDINES AND SUBSTITUTED PURINES AND THEIR USE AS UBIQUITIN-SPECIFIC-PROCESSING PROTEASE 1 (USP1) INHIBITORS
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Paragraph 0511, (2020/07/14)
The present disclosure provides compounds having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein X1, X2, X11, X12, R1, R3, R5, R5', R6, and R7 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to inhibit a USP1 protein and/or to treat a disorder responsive to the inhibition of USP1 proteins and USP1 activity. Compounds of the present disclosure are especially useful for treating cancer.
Fluorescent organic light emitting elements having high efficiency
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Page/Page column 90, (2019/07/12)
An organic light-emitting element which emits delayed fluorescence comprising specifically substituted 1,2,4-triazole derivatives, 1,2,4-oxadiazole derivatives or 1,2,4-thiadiazole derivatives in the light-emitting layer, a light-emitting layer comprising
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology
Boga, Sobhana Babu,Deng, Yongqi,Zhu, Liang,Nan, Yang,Cooper, Alan B.,Shipps, Gerald W.,Doll, Ronald,Shih, Neng-Yang,Zhu, Hugh,Sun, Robert,Wang, Tong,Paliwal, Sunil,Tsui, Hon-Chung,Gao, Xiaolei,Yao, Xin,Desai, Jagdish,Wang, James,Alhassan, Abdul Basit,Kelly, Joseph,Patel, Mehul,Muppalla, Kiran,Gudipati, Subrahmanyam,Zhang, Li-Kang,Buevich, Alexei,Hesk, David,Carr, Donna,Dayananth, Priya,Black, Stuart,Mei, Hong,Cox, Kathleen,Sherborne, Bradley,Hruza, Alan W.,Xiao, Li,Jin, Weihong,Long, Brian,Liu, Gongjie,Taylor, Stacey A.,Kirschmeier, Paul,Windsor, William T.,Bishop, Robert,Samatar, Ahmed A.
supporting information, p. 761 - 767 (2018/06/25)
The emergence and evolution of new immunological cancer therapies has sparked a rapidly growing interest in discovering novel pathways to treat cancer. Toward this aim, a novel series of pyrrolidine derivatives (compound 5) were identified as potent inhibitors of ERK1/2 with excellent kinase selectivity and dual mechanism of action but suffered from poor pharmacokinetics (PK). The challenge of PK was overcome by the discovery of a novel 3(S)-thiomethyl pyrrolidine analog 7. Lead optimization through focused structure-activity relationship led to the discovery of a clinical candidate MK-8353 suitable for twice daily oral dosing as a potential new cancer therapeutic.
Colchicine derivatives, and preparation method and medical application thereof
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Paragraph 0092; 0093; 0222; 0224; 0225, (2018/09/14)
The invention specifically relates to colchicine derivatives (I) as described in the specification and a preparation method thereof, and pharmaceutical compositions containing the colchicine derivatives, belonging to the field of medicinal chemistry. The results of pharmacodynamic experiments prove that the colchicine derivatives of the invention have treatment effect on lumbar disc herniation andliver fibrosis.
A 2 - (4 - bromophenyl) -4 - biphenyl -6 - phenyl pyrimidine synthesis method (by machine translation)
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Paragraph 0010; 0036-0038, (2017/07/22)
The invention belongs to the technical field of organic electroluminescent material, discloses a 2 - (4 - bromophenyl) - 4 - biphenyl - 6 - phenyl pyrimidine synthesis method, the invention organic matter to bromophenylmethyl as raw materials, preparation
SPIROCYCLIC COMPOUNDS
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Paragraph 0235, (2017/07/31)
Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.
AROMATIC HETEROCYCLIC COMPOUND
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Paragraph 0647; 0648, (2015/05/05)
The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.
