- Synthesis and Biological Evaluation of Novel Substituted 4-Anilinoquinazolines as Antitumor Agents
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Eleven novel 4-anilinoquinazoline derivatives were synthesized and evaluated for their in?vitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC50 values of 25?682?nm against various types of cancer cell l
- Cao, Dong,Wang, Xiaoyan,Lei, Lei,Ma, Liang,Yang, Zhuang,Wang, Fang,Chen, Lijuan
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p. 1084 - 1094
(2020/12/02)
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- FLUORESCENT SENSORS OF PEROXYNITRITE TARGETED TO THE ENDOPLASMIC RETICULUM
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A compound can be a pro-fluorophore peroxynitrite sensor that generates a fluorophore when cleaved by peroxynitrite, having a structure of Formula A: wherein: moiety A is an ER-targeting fluorophore; Y is a linker; and moiety B is a phenol, substituted or
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Paragraph 0107
(2019/10/23)
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- HISTONE DEACETYLASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
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A compound represented by Formula I or pharmaceutically acceptable salt thereof. The present invention relates to a 4-arylamino quinazoline hydroxamic acid compound having a histone deacetylase inhibitory activity, preparation method of the compound, pharmaceutical composition comprising the compound, and use of the compound and the pharmaceutical composition in the preparation of a histone deacetylase inhibitor medicine. The present invention aims at acquiring, via a medicine design and a synthetic technology, a series of selective histone deacetylase inhibitors having good hypotype selectivity and favorable pharmacokinetic characteristics based on optimization of an enzyme surface recognition region and connection region of 4-arylamino quinazoline, thus reducing an effect on normal tissues or cells while improving an antineoplastic activity of the normal tissues or cells.
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Paragraph 0230-0231
(2018/04/20)
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- Bismuth trichloride–mediated cleavage of phenolic methoxymethyl ethers
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A simple and efficient method for removal of phenolic methoxymethyl ethers in the presence of 30?mol% of bismuth trichloride in acetonitrile/water is described. Notable features of the cleavage protocol entail use of an ecofriendly bismuth reagent, ease of handling, low cost, operational simplicity, and good functional group compatibility. A number of structurally varied phenolic methoxymethyl ethers were cleaved in good to excellent yields.
- Obaro-Best, Oghale,Reed, Jack,Norfadilah, Alya A. F. B.,Monahan, Ryan,Sunasee, Rajesh
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supporting information
p. 586 - 593
(2016/06/08)
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- Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer
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Novel selective histone deacetylase 6 (HDAC6) inhibitors using the quinazoline as the cap were designed, synthesized, and evaluated for HDAC enzymatic assays. N-Hydroxy-4-(2-methoxy-5-(methyl(2-methylquinazolin-4-yl)amino)phenoxy)butanamide, 23bb, was the
- Yang, Zhuang,Wang, Taijin,Wang, Fang,Niu, Ting,Liu, Zhuowei,Chen, Xiaoxin,Long, Chaofeng,Tang, Minghai,Cao, Dong,Wang, Xiaoyan,Xiang, Wei,Yi, Yuyao,Ma, Liang,You, Jingsong,Chen, Lijuan
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p. 1455 - 1470
(2016/03/08)
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- A histone deacetylase inhibitor and its preparation and use (by machine translation)
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The invention provides a compound of formula I illustrated compound or its pharmaceutically acceptable salt, relates to has the histone deacetylase inhibitory activity of the 4 - aryl amino [...] novel class of compound, the preparation of the compounds, comprising the pharmaceutical composition and the compounds and pharmaceutical compositions in the preparation of histone deacetylase enzyme inhibitor drug in its class of use; aimed at through the drug design and synthesis means based on obtaining a series of 4 - aryl amino [...] surface of the cleat and linkage area optimization, with subtype selective and good medicine generation of dynamics characteristic of selective histone deacetylase inhibitors, in order to improve the anti-tumor activity at the same time to reduce the impact of the normal tissue or cells. (by machine translation)
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Paragraph 0314; 0315; 0332; 0333; 0334; 0335
(2017/02/17)
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- Molecular imaging of peroxynitrite with HKGreen-4 in live cells and tissues
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Peroxynitrite (ONOO-), the product of a radical combination reaction of nitric oxide and superoxide, is a potent biological oxidant involved in a broad spectrum of physiological and pathological processes. Herein we report the development, characterization, and biological applications of a new fluorescent probe, HKGreen-4, for peroxynitrite detection and imaging. HKGreen-4 utilizes a peroxynitrite-triggered oxidative N-dearylation reaction to achieve an exceptionally sensitive and selective fluorescence turn-on response toward peroxynitrite in chemical systems and biological samples. We have thoroughly evaluated the utility of HKGreen-4 for intracellular peroxynitrite imaging and, more importantly, demonstrated that HKGreen-4 can be efficiently employed to visualize endogenous peroxynitrite generated in Escherichia coli-challenged macrophages and in live tissues from a mouse model of atherosclerosis. This probe should serve as a powerful molecular imaging tool to explore peroxynitrite biology under a variety of physiological and pathological contexts.
- Peng, Tao,Wong, Nai-Kei,Chen, Xingmiao,Chan, Yee-Kwan,Ho, Derek Hoi-Hang,Sun, Zhenning,Hu, Jun Jacob,Shen, Jiangang,El-Nezami, Hani,Yang, Dan
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supporting information
p. 11728 - 11734
(2014/10/16)
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- HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 -HYDROXYSTEROID DEHYDROGENASE
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Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
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Page/Page column 125-126
(2010/08/07)
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- Highly efficient and selective methoxymethylation of alcohols and phenols catalyzed by high-valent tin(IV) porphyrin
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An efficient and selective method for methoxymethylation of alcohols and phenols with formaldehyde dimethyl acetal (FDMA) catalyzed by electron deficient tin(IV)tetraphenylporphyrinato trifluoromethanesulfonate, [SnIV(TPP)(OTf)2], is
- Gharaati, Shadab,Moghadam, Majid,Tangestaninejad, Shahram,Mirkhani, Valiollah,Mohammadpoor-Baltork, Iraj,Kosari, Farshid
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experimental part
p. 1995 - 2000
(2011/01/07)
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- Highly efficient and selective methoxymethylation of alcohols and phenols catalyzed by reusable ZrO(OTf)2 under solvent-free conditions
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Different primary, secondary, and tertiary alcohols were efficiently converted to their corresponding methoxymethyl ethers with formaldehyde dimethyl acetal in the presence of catalytic amounts of ZrO(OTf)2 at room temperature. Phenols were als
- Moghadam, Majid,Tangestaninejad, Shahram,Mirkhani, Valiollah,Mohammadpoor-Baltork, Iraj,Khajehzadeh, Mostafa
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experimental part
p. 641 - 647
(2011/05/04)
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- High-valent [SnIV(Br8TPP)(OTf)2] as a highly efficient and reusable catalyst for selective methoxymethylation of alcohols and phenols: The effect of substituted bromines on the catalytic activity
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High-valent tin(IV)octabromotetraphenylporphyrinato trifluoromethanesulfonate, [SnIV(Br8TPP)(OTf)2], was used for selective methoxymethylation of alcohols and phenols with formaldehyde dimethyl acetal (FDMA) at room temper
- Moghadam, Majid,Tangestaninejad, Shahram,Mirkhani, Valiollah,Mohammadpoor-Baltork, Iraj,Khajehzadeh, Mostafa,Kosari, Farshid,Araghi, Mehdi
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experimental part
p. 238 - 243
(2010/04/04)
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- Convenient Method for the ortho-Formylation of Phenols
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Phenolic derivatives are formylated selectively ortho to the hydroxy group by paraformaldehyde with magnesium dichloride-triethylamine as base. With alkyl-substituted phenols excellent yields of the corresponding salicylaldehyde derivatives were obtained. Similar results were obtained with chloro-substituted phenols and with 3- and 4-methoxyphenol, while 2-methoxyphenol was unreactive. A good yield of methyl 3-formyl-4-hydroxybenzoate was obtained by this method as well, but generally phenols with electron-attracting groups reacted sluggishly; the long reaction times required caused the formation of by-products, particularly MOM-derivatives of the phenols.
- Hofslokken, Nini U.,Skattebol, Lars
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p. 258 - 262
(2007/10/03)
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- Methoxymethylation of alcohols, phenols, and avermectin aglycones using MOM-2-pyridylsulfide
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Methoxymethyl-2-pyridylsulfide (MOM-ON) is an effective methoxymethylating reagent when used in conjunction with AgOTf, NaOAc, and THF. A wide range of MOM ethers are produced from corresponding phenols and alcohols, including tertiary and allylic alcohols, in good yields and under mild, neutral conditions. This method is also effective for the methoxymethylation of avermectin aglycones.
- Marcune,Karady,Dolling,Novak
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p. 2446 - 2449
(2007/10/03)
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