Pub Date : 2021-09-19DOI: 10.25135/acg.oc.112.21.07.2139
R. Erenler, Murat Sünkür, S. Aydin, Tarık Aral, B. Dag
{"title":"Preparation of new mono- and bis-amide derivatives of L-isoleucine via amidation of carboxyl and amino groups","authors":"R. Erenler, Murat Sünkür, S. Aydin, Tarık Aral, B. Dag","doi":"10.25135/acg.oc.112.21.07.2139","DOIUrl":"https://doi.org/10.25135/acg.oc.112.21.07.2139","url":null,"abstract":"","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2021-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45412254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-09-19DOI: 10.25135/acg.oc.111.21.06.2118
M. Gümüş, Selin Can, H. Eroğlu, İ. Koca
{"title":"Synthesis of novel salicylic acid-pyrrolone conjugates and investigation of their cytotoxic and genotoxic effects in Allium cepa root tip cells","authors":"M. Gümüş, Selin Can, H. Eroğlu, İ. Koca","doi":"10.25135/acg.oc.111.21.06.2118","DOIUrl":"https://doi.org/10.25135/acg.oc.111.21.06.2118","url":null,"abstract":"","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":"1 1","pages":""},"PeriodicalIF":1.7,"publicationDate":"2021-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41364409","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-06-22DOI: 10.25135/acg.oc101.21.04.2029
I. Gülçin, A. Maharramov, M. Kurbanova, Parham Taslimi, Yeliz Demir, E. Huseyinov, A. Sujayev, S. Alwasel, A. Safarova
{"title":"Synthesis, characterization, crystal structure and bioactivities of novel enamine and pyrrole derivatives endowed with acetylcholinesterase, α-glycosidase and human carbonic anhydrase inhibition effects","authors":"I. Gülçin, A. Maharramov, M. Kurbanova, Parham Taslimi, Yeliz Demir, E. Huseyinov, A. Sujayev, S. Alwasel, A. Safarova","doi":"10.25135/acg.oc101.21.04.2029","DOIUrl":"https://doi.org/10.25135/acg.oc101.21.04.2029","url":null,"abstract":"","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2021-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44846115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-03-26DOI: 10.25135/ACG.OC.99.21.01.1948
Krishnappa B Badiger, Kantharaju Kamanna
This paper present a novel Knoevenagel reaction protocol for the condensation of aromatic/heteroaromatic aldehydes with malononitrile to give α, β–unsaturated benzylidene derivatives. The main focus of this work is to reveal the usability of agro-waste extracts as a catalyst in the Knoevenagel condensation. The present protocol proceeds efficiently for various substituted aromatic and heterocyclic aldehydes in the Knoevenagel reactions. In addition, the present method describes direct isolation of the formed products without using organic solvent extraction gave good yields product.
{"title":"Knoevenagel condensation reaction catalysed by agro-waste extract as a greener solvent catalyst","authors":"Krishnappa B Badiger, Kantharaju Kamanna","doi":"10.25135/ACG.OC.99.21.01.1948","DOIUrl":"https://doi.org/10.25135/ACG.OC.99.21.01.1948","url":null,"abstract":"This paper present a novel Knoevenagel reaction protocol for the condensation of aromatic/heteroaromatic aldehydes with malononitrile to give α, β–unsaturated benzylidene derivatives. The main focus of this work is to reveal the usability of agro-waste extracts as a catalyst in the Knoevenagel condensation. The present protocol proceeds efficiently for various substituted aromatic and heterocyclic aldehydes in the Knoevenagel reactions. In addition, the present method describes direct isolation of the formed products without using organic solvent extraction gave good yields product.","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2021-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41844410","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-26DOI: 10.25135/acg.oc.86.20.10.1853
Cenk A Andac
Herein, a facile procedure for microwave synthesis and NMR characterization of phenothiazine derivatives 10-(3-hydroxypropyl)-2-(methylsulphanyl)-10H-phenothiazine (3) (25% yield) and 1-[3-(2-methylsulfanyl-10H-phenothiazine-10-yl)-propyl]pyrimidine-2,4-(1H,3H)-dione (6) (67% yield) is described. After successful microwave synthesis steps, MTT cytotoxicity experiments gave rise to greater anticancer effect of compound 6 in MCF-7 human breast adenocarcinoma cell line (IC50= 1.35 µM) as compared to literature values for tamoxifen (IC50= 8.3 µM) and doxorubicin (IC50= 27 µM).
{"title":"Facile microwave synthesis of a novel phenothiazine derivative and its cytotoxic activity","authors":"Cenk A Andac","doi":"10.25135/acg.oc.86.20.10.1853","DOIUrl":"https://doi.org/10.25135/acg.oc.86.20.10.1853","url":null,"abstract":"Herein, a facile procedure for microwave synthesis and NMR characterization of phenothiazine derivatives 10-(3-hydroxypropyl)-2-(methylsulphanyl)-10H-phenothiazine (3) (25% yield) and 1-[3-(2-methylsulfanyl-10H-phenothiazine-10-yl)-propyl]pyrimidine-2,4-(1H,3H)-dione (6) (67% yield) is described. After successful microwave synthesis steps, MTT cytotoxicity experiments gave rise to greater anticancer effect of compound 6 in MCF-7 human breast adenocarcinoma cell line (IC50= 1.35 µM) as compared to literature values for tamoxifen (IC50= 8.3 µM) and doxorubicin (IC50= 27 µM).","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2020-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44717527","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-26DOI: 10.25135/acg.oc.89.20.05.1660
Sule Un, R. Altundas, A. Gören
The synthesis of precursors of neurotoxic ɣ-glutamyl β-cyanoalanine was developed starting from L-Serine via through the preparation of b-cyanoalanine and glutamyl units. Coupling of these two intermediates gave methyl ester of ɣ-glutamyl β-cyanoalanine precursor.
{"title":"Synthesis of ɣ-glutamyl β-cyanoalanine precursor","authors":"Sule Un, R. Altundas, A. Gören","doi":"10.25135/acg.oc.89.20.05.1660","DOIUrl":"https://doi.org/10.25135/acg.oc.89.20.05.1660","url":null,"abstract":"The synthesis of precursors of neurotoxic ɣ-glutamyl β-cyanoalanine was developed starting from L-Serine via through the preparation of b-cyanoalanine and glutamyl units. Coupling of these two intermediates gave methyl ester of ɣ-glutamyl β-cyanoalanine precursor.","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2020-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45103958","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-26DOI: 10.25135/acg.oc.85.20.08.1768
Parshuram M. Pisal, V. T. Kamble, Dr. Ravi Varala, Pradip B. Gujarathi
Tetrabutylammonium bromide (TBAB) and cesium carbonate (Cs2O3) catalyzed, one-pot three-component synthesis of 2H-indazole[2,1b]phthalazine-1,6,11(13H)-triones was developed at room temperature in ethanol. Both electron donating and withdrawing groups are compatible under the optimized reaction parameters.
{"title":"Efficient one-pot three-component synthesis of 2H-indazole [2,1-b]phthalazine-1,6,11(13H)-triones at room temperature","authors":"Parshuram M. Pisal, V. T. Kamble, Dr. Ravi Varala, Pradip B. Gujarathi","doi":"10.25135/acg.oc.85.20.08.1768","DOIUrl":"https://doi.org/10.25135/acg.oc.85.20.08.1768","url":null,"abstract":"Tetrabutylammonium bromide (TBAB) and cesium carbonate (Cs2O3) catalyzed, one-pot three-component synthesis of 2H-indazole[2,1b]phthalazine-1,6,11(13H)-triones was developed at room temperature in ethanol. Both electron donating and withdrawing groups are compatible under the optimized reaction parameters.","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2020-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46973524","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-26DOI: 10.25135/acg.oc.88.20.11.1870
N. Korol, M. Slivka, O. Holovko-Kamoshenkova
The sources, describing cycloaddition reactions with the participation of 4-phenyl-3H-1,2,4-triazole-3,5(4H)-dione (PTAD) and 4-methyl-3H-1,2,4-triazole-3,5(4H)-dione (MTAD) were reviewed from the middle 1970s and they are mentioned in chronological order. It was noted that the most investigated are Diels-Alder reactions and cycloaddition to a few cyclic mono- and dienes. Stereochemistry of obtained products are also described.
{"title":"Cycloaddition reactions of 4-phenyl-3H-1,2,4-triazole-3,5(4H)-dione (PTAD) and 4-methyl-3H-1,2,4-triazole-3,5(4H)-dione (MTAD): A short review","authors":"N. Korol, M. Slivka, O. Holovko-Kamoshenkova","doi":"10.25135/acg.oc.88.20.11.1870","DOIUrl":"https://doi.org/10.25135/acg.oc.88.20.11.1870","url":null,"abstract":"The sources, describing cycloaddition reactions with the participation of 4-phenyl-3H-1,2,4-triazole-3,5(4H)-dione (PTAD) and 4-methyl-3H-1,2,4-triazole-3,5(4H)-dione (MTAD) were reviewed from the middle 1970s and they are mentioned in chronological order. It was noted that the most investigated are Diels-Alder reactions and cycloaddition to a few cyclic mono- and dienes. Stereochemistry of obtained products are also described.","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2020-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48346142","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-26DOI: 10.25135/acg.oc.91.20.11.1913
Hülya Yanık, Sümeyra Ayan, A. Akdemir, Ö. Erdoğan, C. B. Ustundag, O. Cevik, Ozgur Yilmaz
Quinones, especially 1,4-naphthoquinones, are one of the most significant and widely distributed phytochemical groups in nature. 1,4-Naphthoquinones and their synthetic derivatives are found to possess remarkable cytotoxic activities. In this study, a series of 2-aminonaphtho[2,3-d][1,3]thiazole-4,9-dione derivatives were synthesized and their structures were verified with spectral analysis. In vitro cytotoxic activities of the synthesized compounds were evaluated by using MTT assay against MKN-45 (Human Gastric cancer), MDA-MB-231 (Human Breast cancer) and HeLa (Human Cervical cancer) cell lines. Among the synthesized compounds, 3d inhibited MDA-MB-cell proliferation with an IC50 value of 0.276 µM. Compound 3a inhibited HeLa and MKN-45 cell proliferation with IC50 values of 0.336 µM and 8.769 µM, respectively. Compound 3b inhibited HELA cell proliferation with an IC50 value of 0.269 µM. Molecular docking results suggest that the ligands may bind to the hDNA TopoIIβ binding pocket and partially exert their effects. These results propose that 2-aminonaphtho[2,3-d]thiazole-4,9-dion core has important biological effects and further explorations are worthwhile.
{"title":"Synthesis, anticancer activities and molecular modeling studies of some 2-aminonaphtho[2,3-d][1,3]thiazole-4,9-dione derivatives","authors":"Hülya Yanık, Sümeyra Ayan, A. Akdemir, Ö. Erdoğan, C. B. Ustundag, O. Cevik, Ozgur Yilmaz","doi":"10.25135/acg.oc.91.20.11.1913","DOIUrl":"https://doi.org/10.25135/acg.oc.91.20.11.1913","url":null,"abstract":"Quinones, especially 1,4-naphthoquinones, are one of the most significant and widely distributed phytochemical groups in nature. 1,4-Naphthoquinones and their synthetic derivatives are found to possess remarkable cytotoxic activities. In this study, a series of 2-aminonaphtho[2,3-d][1,3]thiazole-4,9-dione derivatives were synthesized and their structures were verified with spectral analysis. In vitro cytotoxic activities of the synthesized compounds were evaluated by using MTT assay against MKN-45 (Human Gastric cancer), MDA-MB-231 (Human Breast cancer) and HeLa (Human Cervical cancer) cell lines. Among the synthesized compounds, 3d inhibited MDA-MB-cell proliferation with an IC50 value of 0.276 µM. Compound 3a inhibited HeLa and MKN-45 cell proliferation with IC50 values of 0.336 µM and 8.769 µM, respectively. Compound 3b inhibited HELA cell proliferation with an IC50 value of 0.269 µM. Molecular docking results suggest that the ligands may bind to the hDNA TopoIIβ binding pocket and partially exert their effects. These results propose that 2-aminonaphtho[2,3-d]thiazole-4,9-dion core has important biological effects and further explorations are worthwhile.","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2020-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46107876","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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