- Antihyperlipidemic studies of newly synthesized phenolic derivatives: In silico and in vivo approaches
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Background: Hyperlipidemia is a worth-mentioning risk factor in quickly expanding cardiovascular diseases, including myocardial infarction and, furthermore, in stroke. Methods: The present work describes the synthesis of phenolic derivatives 4a–e and 6a–c
- Aqeel, Muhammad Tahir,Ur-Rahman, Nisar,Khan, Arif-Ullah,Ashraf, Zaman,Latif, Muhammad,Rafique, Hummera,Rasheed, Usman
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Read Online
- Synthesis and biological evaluation of novel hybrids of phenylsulfonyl furoxan and phenstatin derivatives as potent anti-tumor agents
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Hybridization of nitric oxide (NO) donors with known anti-cancer agents have been emerged as a strategy to achieve improved therapeutic effect and to overcome chemo-resistance in cancer therapy. In this study, furoxan moiety as an efficient NO donor was i
- Huang, Xin,Wang, Yu-Shuang,Ma, Duo,Wang, Yuan-Yuan,Bian, Shi-Da,Zhang, Bo,Qiao, Yu,He, Zi-Ran,Lv, Meng,Cai, Guo-Long,Wang, Zi-Xuan,Liu, Xue-Song,Shi, Jing-Bo,Liu, Ming-Ming
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- PROCESS FOR THE PREPARATION OF 4,5-DIHYDROXY-2-(4-METHYLBENZYL)ISOPHTHALONITRILE
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The present disclosure relates to a process for the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile, to use of a compound which is 2-methoxy-5-(4-methylbenzyl)phenol, (3-hydroxy-4-methoxyphenyl)(p-tolyl)methanone, 2-methoxy-5-(4-methylben
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Page/Page column 13
(2020/06/03)
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- Novel ketoprofen–antioxidants mutual codrugs as safer nonsteroidal anti-inflammatory drugs: Synthesis, kinetic and pharmacological evaluation
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Ketoprofen belongs to one of the most common nonsteroidal anti-inflammatory drugs (NSAIDs) but its clinical usefulness has been restricted due to the high incidence of gastrointestinal complications. The release of reactive oxygen species (ROS) in NSAIDs
- Sehajpal, Shikha,Prasad, Deo Nandan,Singh, Rajesh K.
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- Substituted phenyl[(5-benzyl-1,3,4-oxadiazol-2-yl)sulfanyl]acetates/acetamides as alkaline phosphatase inhibitors: Synthesis, computational studies, enzyme inhibitory kinetics and DNA binding studies
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Substituted phenyl[(5-benzyl-1,3,4-oxadiazol-2-yl)sulfanyl]acetates/acetamides 9a-j were synthesized as alkaline phosphatase inhibitors. Phenyl acetic acid 1 through a series of reactions was converted into 5-benzyl-1,3,4-oxadiazole-2-thione 4. The intermediate oxadiazole 4 was then reacted with chloroacetyl derivatives of phenols 6a-f and anilines derivatives 8a-d to afford the title oxadiazole derivatives 9a-j. All of the title compounds 9a-j were evaluated for their inhibitory activity against human alkaline phosphatise (ALP). It was found that compounds 9a-j exhibited good to excellent alkaline phosphatase inhibitory activity especially 9h displayed potent activity with IC50 value 0.420 ± 0.012 μM while IC50 value of standard (KH2PO4) was 2.80 μM. The enzyme inhibitory kinetics of most potent inhibitor 9h was determined by Line-weaever Burk plots showing non-competitive mode of binding with enzyme. Molecular docking studies were performed against alkaline phosphatase enzyme (1EW2) to check the binding affinity of the synthesized compounds 9a-j against target protein. The compound 9h exhibited excellent binding affinity having binding energy value (?7.90 kcal/mol) compared to other derivatives. The brine shrimp viability assay results proved that derivative 9h was non-toxic at concentration used for enzyme assay. The lead compound 9h showed LD50 106.71 μM while the standard potassium dichromate showed LD50 0.891 μM. The DNA binding interactions of the synthesized compound 9h was also determined experimentally by spectrophotometric and electrochemical methods. The compound 9h was found to bind with grooves of DNA as depicted by both UV–Vis spectroscopy and cyclic voltammetry with binding constant values 7.83 × 103 and 7.95 × 103 M?1 respectively revealing significant strength of 9h-DNA complex. As dry lab and wet lab results concise each other it was concluded that synthesized compounds, especially compound 9h may serve as lead compound to design most potent inhibitors of human ALP.
- Iqbal,Ashraf,Hassan, Mubashir,Abbas,Jabeen, Erum
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- Synthesis and evaluation of prodrugs of ketoprofen with antioxidants as gastroprotective NSAIDs
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Ketoprofen-antioxidant mutual prodrugs were synthesized to reduce the gastrointestinal effects associated with ketoprofen. For reducing the gastrointestinal toxicity, the free carboxylic group (–COOH) was temporarily masked by esterification with alcoholi
- Sehajpal, Shikha,Prasad, Deo Nandan,Singh, Rajesh K.
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p. 2145 - 2150
(2018/08/09)
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- Supercritical fluid chromatography approach for a sustainable manufacture of new stereoisomeric anticancer agent
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Two routes aimed at the manufacture of unprecedented stereoisomeric combretastatin A-4 analogue were described: flash chromatography vs supercritical fluid chromatography. The latter has many advantages over liquid chromatography and was therefore chosen for the small scale separation of methyl 1-[(3-hydroxy-4-methoxyphenyl) (3,4,5-trimethoxyphenyl)methyl]-5-oxo-L-prolinate 5, with potential antitumoral activity. After a screening of six different polysaccharide based chiral stationary phases and four co-solvents, the percentage of co-solvent, the flow-rate and the outlet pressure were optimized through a design of experiments (DoE). The preparation of 50 mg of each stereoisomer was achieved successfully on a Chiralpak AD-H with isopropanol as a co-solvent. Productivity (kkd), solvent usage and environmental factor (E Factor) were calculated. Flash chromatography and supercritical fluid chromatography approaches were compared in terms of yield and purity of each stereoisomer manufactured.
- Ghinet, Alina,Zehani, Yasmine,Lipka, Emmanuelle
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p. 845 - 853
(2017/08/22)
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- Preparation method of 3-hydroxyl-4-methoxyl-4'-methylbenzophenone
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The invention relates to a preparation method of 3-hydroxyl-4-methoxyl-4'-methylbenzophenone. The preparation method comprises the following steps that (1) o-methoxyphenol and acyl chloride react to generate a compound I under the existence of solvents an
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Paragraph 0030; 0032; 0033; 0034; 0042; 0049
(2017/11/16)
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- Benzophenone-nucleoside derivatives as telomerase inhibitors: Design, synthesis and anticancer evaluation in vitro and in vivo
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Based on telomerase, thirteen novel phenstatin moiety linked stavudine derivatives (8a~8e and 11a~11f) were synthesized. The structures were determined by NMR and TOF-HRMS. The screening results showed that some compounds had better anti-cancer activity i
- Shi, Jing Bo,Chen, Liu Zeng,Wang, Yang,Xiou, Cheng,Tang, Wen Jian,Zhou, Hai Pin,Liu, Xin Hua,Yao, Qi Zheng
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p. 729 - 739
(2016/09/23)
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- Synthesis and evaluation of antioxidant-S-(+)-ibuprofen hybrids as gastro sparing NSAIDs
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Ibuprofen is one of the most popular NSAIDs for the last three decades but also known for its gastrointestinal side effects similar to other NSAIDs. To overcome this problem, we have designed and synthesized ibuprofen - antioxidant (thymol, guaiacol, eugenol, and menthol) hybrids (6-13) with and without spacer as gastro sparing agents. The hybrids have been found to be chemically stable, biolabile and exhibited retention of anti-inflammatory and analgesic activity with significant reduced ulcerogenicity as compared to the ibuprofen and ibuprofen + antioxidant physical mixture. The absence of ulcerogenicity may be attributed to antioxidants and improved physicochemical properties of these hybrid molecules.
- Chandiran, Senthil,Vyas, Sandeep,Sharma, Neetika,Sharma, Manu
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p. 1006 - 1016
(2014/01/06)
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- New efficient synthesis of combretastatin A-4 via Colvin rearrangement
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A new four-step approach for the synthesis of anticancer agent combretastatin A-4 (CA-4) has been developed. The method includes the Colvin rearrangement of the benzophenone derivative phenstatin to the key diarylalkyne followed by stereoselective semi-reduction to CA-4 in good overall yield.
- Petrov, Ognyan I.,Gerova, Mariana S.,Chanev, Christo D.,Petrova, Katya V.
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scheme or table
p. 3711 - 3715
(2011/12/15)
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- Synthesis and biological evaluation of phenstatin metabolites
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Previous investigations on the incubation of phenstatin with rat and human microsomal fractions revealed the formation of nine main metabolites. The structures of eight of these metabolites have been now confirmed by synthesis and their biological properties have been reported. Eaton's reagent was utilized as a convenient condensing agent, allowing, among others, a simple multigram scale preparation of phenstatin. Synthesized metabolites and related compounds were evaluated for their antiproliferative activity in the NCI-60 cancer cell line panel, and for their effect on microtubule assembly. Metabolite 23 (2′-methoxyphenstatin) exhibited the most potent in vitro cytotoxic activity: inhibition of the growth of K-562, NCI-H322M, NCI-H522, KM12, M14, MDA-MB-435, NCI/ADR-RES, and HS 578T cell lines with GI50 values 50 = 3.2 μM vs 15.0 μM) and induced G2/M arrest in murine leukemia DA1-3b cells. The identification of this active metabolite led to the design and synthesis of analogs with potent in vitro cytotoxicity and inhibition of microtubule assembly.
- Ghinet, Alina,Rigo, Beno?t,Hénichart, Jean-Pierre,Le Broc-Ryckewaert, Delphine,Pommery, Jean,Pommery, Nicole,Thuru, Xavier,Quesnel, Bruno,Gautret, Philippe
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supporting information; experimental part
p. 6042 - 6054
(2011/11/29)
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- Design, synthesis and evaluation of diclofenac-antioxidant mutual prodrugs as safer NSAIDs
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Diclofenac has been conjugated with different antioxidants having antiulcerogenic activity with the objective of obtaining diclofenac-antioxidant mutual prodrugs as safer NSAIDs devoid of ulcerogenic side-effects. The synthesized derivatives are screened
- Manon, Benu,Sharma, Pritam D.
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experimental part
p. 1279 - 1287
(2010/02/27)
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- Mutual prodrugs of 4-biphenylacetic acid and phytophenolics as safer NSAIDs - Synthetic and spectral studies
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4-Biphenylacetic acid (4-BPA), the active metabolite of NSAID fenbufen has been modified using mutual prodrug approach. Number of 4-BPA derivatives have been synthesised as potential mutual prodrugs by the attachment of several phytophenols/alcohol as pro
- Sharma, Pritam Dev,Kaur, Gurbinder,Kansal, Sumeet,Chandiran, Senthil Kumar
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p. 2159 - 2164
(2007/10/03)
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- Ortho-Coordinated Acylation on Phenol Systems
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The ortho-coordinated acylation of phenol salts reported in recent synthetic applications has been extensively investigated.The data obtained support the hypothesis that formation of an organized complex between the phenol salts and the acylating agents may strongly influence the reaction pathway, depending on the nature of the specific cation, phenol, and acyl chloride involved in the process.The structural factors which control the formation of the reacting complex 3 have been extensively investigated; the results obtained allow us to discuss the possibilities and limitations of this methodology in selective o-acylphenol synthesis.The present methodology is the procedure of choice for ortho-functionalization of phenols with electrophilic reagents such as phosgene, oxaloyl chlorides, polyunsaturated acid chlorides, phthalic dichlorides, and, in general, acid chlorides α-functionalized with an electron-withdrawing group.
- Sartori, Giovanni,Casnati, Giuseppe,Bigi, Franca
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p. 4371 - 4377
(2007/10/02)
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