- Design, synthesis and biological evaluation of anilide (dicarboxylic acid) shikonin esters as antitumor agents through targeting PI3K/Akt/mTOR signaling pathway
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Triple-negative breast cancer (TNBC) has an unfavorable prognosis attribute to its low differentiation, rapid proliferation and high distant metastasis rate. PI3K/Akt/mTOR as an intracellular signaling pathway plays a key role in the cell proliferation, m
- Ma, Yingying,Yang, Xiaorong,Han, Hongwei,Wen, Zhongling,Yang, Minkai,Zhang, Yahan,Fu, Jiangyan,Wang, Xuan,Yin, Tongming,Lu, Guihua,Qi, Jinliang,Lin, Hongyan,Wang, Xiaoming,Yang, Yonghua
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- N-Aryl Amides as Chemical Exchange Saturation Transfer Magnetic Resonance Imaging Contrast Agents
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Chemical exchange saturation transfer (CEST) MRI has recently emerged as a versatile molecular imaging approach in which diamagnetic compounds can be utilized to generate an MRI signal. To expand the scope of CEST MRI applications, herein, we systematical
- Cai, Xuekang,Zhang, Jia,Lu, Jiaqi,Yi, Long,Han, Zheng,Zhang, Shuixing,Yang, Xing,Liu, Guanshu
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supporting information
p. 11705 - 11709
(2020/08/13)
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- Synthesis, characterization crystal structures and DNA binding studies of zinc complexes with oxygen and nitrogen donor ligands
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Three zinc metal complexes viz, [Zn(L1)2phen] (1), [Zn2(L2)4(bipy)2] (2) and [Zn(L2)2bipy·H2O] (3) where HL1 = 4-(o-toluidino)-4-oxobutanoic acid
- Mehr-un-Nisa,Sirajuddin, Muhammad,Ali, Saqib,Tahir, Muhammad Nawaz,Iqbal, Muhammad
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- An expeditious synthesis of imides from phthalic, maleic and succinic anhydrides and chemoselective C=C reduction of maleic amide esters
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Phthalic, maleic and succinic anhydrides have been reacted with aromatic amines to obtain the corresponding monoacid monoamides. The latter have been each transformed into the corresponding cyclic imide derivatives by treating with SOCl2. Alternatively, anhydrides have been reacted with methanolic KOH to obtain monomethyl ester derivatives which on reaction with aromatic amines in the presence of EDC. HCl and HOBt give cyclic imide derivatives. Reaction of monoacid monoamides independently, with SOCl 2 at 0-5°C give the monoamide monoester derivatives. Treatment of monoamide monoester of malic anhydride with NaBH4 leads to the unusual reduction of C=C grouping as well as the carbonyl group of the ester group to from monoamide monoalcohol of succinic anhydride. Preparation of monoamide monoalcohol of succinic anhydride can also be achieved by chemoselective reduction of monoamide monoester of malic anhydride with Mg turnings yielding monoamide monoester of succinic anhydride followed by reduction of the latter with NaBH4.
- Kumar, Padam Praveen,Reddy, Y. Dathu,Kumari, Y. Bharathi,Devi, B. Rama,Dubey
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p. 392 - 398
(2014/05/06)
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- A facile and green synthesis of N-substituted imides
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Anhydrides 1, 6 and 10 have been reacted, independently, with aromatic primary amines 2 in solid phase by simple physical grinding of reactants with p-toluenesulphonicacid as a catalyst to yield corresponding open chain derivatives, monoacid monoamides3,7 and 11 respectively. The latter have each been transformed into the corresponding cyclic derivatives, i.e. imides 5, 9 and 13 respectively in solid phase by simple physical grinding of each with K 2CO3, alkylating agent and tetrabutylammoniumbromide as a catalyst with short reaction times. These cyclic imides can also be obtained by physical grinding of each of 3, 7 and 11 with dicyclohexylcarbodimide as a dehydrating agent in solid phase.
- Kumar, Padam Praveen,Rama Devi,Dubey
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p. 1166 - 1171
(2013/09/24)
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- Ligand-based modelling followed by synthetic exploration unveil novel glycogen phosphorylase inhibitory leads
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Glycogen phosphorylase (GP) is a valid anti-diabetic target. Accordingly, we applied a drug discovery workflow to unveil novel inhibitory GP leads via combining pharmacophore modeling, QSAR analysis and in silico screening, followed by synthetic exploration of active hits. Virtual screening identified six low micromolar inhibitory leads from the National Cancer Institute (NCI) list of compounds. The most potent hits exhibited anti-GP IC50 values of 3.2 and 4.1 μM. Synthetic exploration of hit 59 (IC50 = 4.1 μM) yielded 25 lead inhibitors with the best illustrating IC50 of 3.0 μM. Interestingly, we prepared several novel mixed oxalyl amide anti-GP leads employing new chemical reaction involving succinic acid-based adducts.
- Habash, Maha,Taha, Mutasem O.
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experimental part
p. 4746 - 4771
(2011/09/20)
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- A simple key for benzylic mono- and gem-dibromination of primary aromatic amine derivatives using molecular bromine1
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Quantitative benzylic mono- and gem-dibromination on primary aromatic amine derivatives have been achieved using molecular bromine and by protecting the amino group as a succinimide moiety. The reactions of N-(o/m/p-tolyl)succinimides 5a-c with 1.25 equiv
- Kar, Anirban,Argade, Narshinha P.
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p. 221 - 224
(2007/10/03)
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- Reactions of cyclic anhydrides with aromatic primary amines: Part 3 - Synthesis of novel 3-(N-arylcarbamoyl)- and 3-(N-naphthylcarbamoyl)carboxylic acids
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Some hitherto unreported 3-(N-arylcarbamoyl)propenoic acids 7a-h and 3-(N-naphthylcarbamoyl)propenoic acid 9 have been synthesized in excellent yields, together with some propanoic acid analogues 11a-h and 12 as potential pesticides. Structural assignments of the products are based on elemental analyses and spectral (IR, 1H NMR, mass) data.
- Omuaru, V. O. T.
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p. 814 - 816
(2007/10/03)
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