Jeremy A Arbesfeld, Estelle Y Da, James S Stevenson, Kori Kuzma, Anika Paul, Tierra Farris, Benjamin J Capodanno, Sally B Grindstaff, Kevin Riehle, Nuno Saraiva-Agostinho, Jordan F Safer, Aleksandar Milosavljevic, Julia Foreman, Helen V Firth, Sarah E Hunt, Sumaiya Iqbal, Melissa S Cline, Alan F Rubin, Alex H Wagner
{"title":"Mapping MAVE data for use in human genomics applications.","authors":"Jeremy A Arbesfeld, Estelle Y Da, James S Stevenson, Kori Kuzma, Anika Paul, Tierra Farris, Benjamin J Capodanno, Sally B Grindstaff, Kevin Riehle, Nuno Saraiva-Agostinho, Jordan F Safer, Aleksandar Milosavljevic, Julia Foreman, Helen V Firth, Sarah E Hunt, Sumaiya Iqbal, Melissa S Cline, Alan F Rubin, Alex H Wagner","doi":"10.1101/2023.06.20.545702","DOIUrl":"10.1101/2023.06.20.545702","url":null,"abstract":"<p><p>The large-scale experimental measures of variant functional assays submitted to MaveDB have the potential to provide key information for resolving variants of uncertain significance, but the reporting of results relative to assayed sequence hinders their downstream utility. The Atlas of Variant Effects Alliance mapped multiplexed assays of variant effect data to human reference sequences, creating a robust set of machine-readable homology mappings. This method processed approximately 2.5 million protein and genomic variants in MaveDB, successfully mapping 98.61% of examined variants and disseminating data to resources such as the UCSC Genome Browser and Ensembl Variant Effect Predictor.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"7 1","pages":""},"PeriodicalIF":1.2,"publicationDate":"2024-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11230167/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72720948","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Alexander V. Komkov, Leonid G. Menchikov, Andrey S. Dmitrenok, Natalya G. Kolotyrkina, Igor V. Zavarzin
{"title":"3-Spiroandrostene-substituted 1,3,4-thiadiazolines","authors":"Alexander V. Komkov, Leonid G. Menchikov, Andrey S. Dmitrenok, Natalya G. Kolotyrkina, Igor V. Zavarzin","doi":"10.1007/s10593-024-03317-z","DOIUrl":"https://doi.org/10.1007/s10593-024-03317-z","url":null,"abstract":"<p>A method for the synthesis of 1,3,4-thiadiazoline spiro steroids <i>via</i> ring A by the reaction of steroid 3-ketones with oxamic acid thiohydrazides was developed. It was shown that if a keto group was present both in ring A and in ring D of the precursor steroid, the reaction occurred only at the keto group of ring A. A number of new steroidal 3-spiroandrostene-substituted 1,3,4-thiadiazolines were obtained, which could be easily acetylated at the thiadiazole NH group.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"48 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141511946","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Alexander V. Komkov, Leonid G. Menchikov, Andrey S. Dmitrenok, Natalya G. Kolotyrkina, Igor V. Zavarzin
{"title":"A method for the synthesis of spiro-1,3,4-thiadiazolines","authors":"Alexander V. Komkov, Leonid G. Menchikov, Andrey S. Dmitrenok, Natalya G. Kolotyrkina, Igor V. Zavarzin","doi":"10.1007/s10593-024-03316-0","DOIUrl":"https://doi.org/10.1007/s10593-024-03316-0","url":null,"abstract":"<p>A method for the synthesis of spiro-1,3,4-thiadiazolines by the reaction of cyclic ketones with oxamic acid thiohydrazides was developed. A number of new nonsteroidal spiro-1,3,4-thiadiazolines was obtained in high yields.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"9 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141511947","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Kirill A. Gomonov, Vasilii V. Pelipko, Igor A. Litvinov, Ruslan I. Baichurin, Sergey V. Makarenko
{"title":"Synthesis and structure of new substituted furan-3-carboxylate hydrazones","authors":"Kirill A. Gomonov, Vasilii V. Pelipko, Igor A. Litvinov, Ruslan I. Baichurin, Sergey V. Makarenko","doi":"10.1007/s10593-024-03308-0","DOIUrl":"https://doi.org/10.1007/s10593-024-03308-0","url":null,"abstract":"<p>The reaction of acetyl-containing furan-3-carboxylates with substituted hydrazines in an alcohol solution leads to the formation of substituted furan-3-carboxylate hydrazones. The resulting hydrazones have <i>E</i>-configuration, as determined by NMR spectroscopy and X-ray diffraction analysis.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"100 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141511948","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Alexei N. Izmest’ev, Sergey S. Isakov, Angelina N. Kravchenko, Galina A. Gazieva
{"title":"The synthesis and antitumor activity of novel 1-alkyl-3-phenyland 3-alkyl-1-phenylimidazothiazolotriazines","authors":"Alexei N. Izmest’ev, Sergey S. Isakov, Angelina N. Kravchenko, Galina A. Gazieva","doi":"10.1007/s10593-024-03318-y","DOIUrl":"https://doi.org/10.1007/s10593-024-03318-y","url":null,"abstract":"<p>Two groups of isomeric imidazothiazolo[1,2,4]triazines and their oxindolylidene derivatives were obtained from 1-alkyl-3-aryl-4,5-dihydroxyimidazolidin-2-(thi)ones. One of the synthesized imidazo[4,5-<i>e</i>]thiazolo[2,3-<i>c</i>][1,2,4]triazine derivatives showed high cytostatic activity at a concentration of 10 μmol/l against four lines of tumor cells: HL-60(TB) (leukemia, –16.1% growth rate), SF-539 (CNS cancer, –2.6% growth rate), MDA-MB-435 (melanoma, –21.2% growth rate), and RXF 393 (kidney cancer, –6.1 % growth rate).</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"21 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141255660","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Vitalii V. Solomin, Darija Zaharova, Aigars Jirgensons
{"title":"Synthesis of 2-arylquinazolines by Chan–Evans–Lam coupling of 2-formylphenylboronic acids with amidines","authors":"Vitalii V. Solomin, Darija Zaharova, Aigars Jirgensons","doi":"10.1007/s10593-024-03314-2","DOIUrl":"https://doi.org/10.1007/s10593-024-03314-2","url":null,"abstract":"<p>A method for the synthesis of 2-arylquinazolines is described which involves Chan–Evans–Lam coupling of 2-formylphenylboronic acids with amidines. The reaction is performed at mild conditions compatible with the range of functional groups and is cost-efficient, provided by usage of inexpensive catalyst and reagents. The synthesis method of 2-arylquinazolines presented is of with scope in both 2-formylphenylboronic acids and amidines.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"70 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141255620","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Diana Y. Pobedinskaya, Oleg P. Demidov, Elena K. Avakyan, Anastasia A. Borovleva, Alexander N. Larin, Artem P. Ermolenko, Ivan V. Borovlev
{"title":"A simple method for the synthesis of diarylamines containing a nitroso group in the ortho position based on the SNH arylamination of 5-nitroisoquinoline","authors":"Diana Y. Pobedinskaya, Oleg P. Demidov, Elena K. Avakyan, Anastasia A. Borovleva, Alexander N. Larin, Artem P. Ermolenko, Ivan V. Borovlev","doi":"10.1007/s10593-024-03313-3","DOIUrl":"https://doi.org/10.1007/s10593-024-03313-3","url":null,"abstract":"<p>A simple and efficient arylamination reaction of 5-nitroisoquinoline based on the oxidative nucleophilic substitution of hydrogen was demonstrated under metal-catalyst-free conditions. This reaction can be used as a method for the synthesis of isoquinoline-based diarylamines containing a nitroso group in the <i>ortho</i> position, which are compounds with high synthetic potential. The oxidation of the latter leads to the formation of 6-arylamino-5-nitroisoquinoline <i>N</i>-oxides. The absence of the need to introduce leaving groups and a good overall yield are features of this reaction.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"36 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141255444","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ravi Varala, Mohan Kurra, Mohammed Amanullah, Mohamed Hussien, Mohammed Mujahid Alam
{"title":"Recent methods in the synthesis of chromeno[2,3-d]pyrimidines","authors":"Ravi Varala, Mohan Kurra, Mohammed Amanullah, Mohamed Hussien, Mohammed Mujahid Alam","doi":"10.1007/s10593-024-03302-6","DOIUrl":"https://doi.org/10.1007/s10593-024-03302-6","url":null,"abstract":"<p>The most recent synthetic methods to produce chromeno[2,3-<i>d</i>]pyrimidine derivatives from 2015 onwards are outlined, and this mini-review is divided into different chapters according to the type of the reaction.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"128 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141255661","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Maxim R. Demidov, Vitaly A. Osyanin, Yury N. Klimochkin
{"title":"An oxidative cleavage of arene-condensed 4H-pyrans via the Grob–Wharton fragmentation","authors":"Maxim R. Demidov, Vitaly A. Osyanin, Yury N. Klimochkin","doi":"10.1007/s10593-024-03310-6","DOIUrl":"https://doi.org/10.1007/s10593-024-03310-6","url":null,"abstract":"<p>When benzannulated dihydroindenochromene and dihydroxanthene derivatives were treated with <i>m</i>-chloroperoxybenzoic acid, oxidative cleavage of the pyran C=C bond and the formation of condensed ketolactones, the derivatives of oxonine-2,6-dione and oxecine-2,7-dione, took place. The reaction proceeded <i>via</i> epoxidation of the pyran double bond followed by the opening of the epoxide and Grob–Wharton fragmentation.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"35 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141255443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dmitry V. Osipov, Pavel E. Krasnikov, Alina A. Artemenko
{"title":"A reaction of 2-carbonyl-substituted 1H-benzo[f]chromenes with N-arylamides of cyanoacetic acid","authors":"Dmitry V. Osipov, Pavel E. Krasnikov, Alina A. Artemenko","doi":"10.1007/s10593-024-03312-4","DOIUrl":"https://doi.org/10.1007/s10593-024-03312-4","url":null,"abstract":"<p>A reaction of 2-trifluoroacetyl-1<i>H</i>-benzo[<i>f</i>]chromenes with <i>N</i>-arylamides of cyanoacetic acid led to the synthesis of a series of 2-oxo-6-trifluoromethylpyridine-3-carboxamides as products of a cascade of the carbo-Michael reaction, Thorpe–Ziegler cyclization, and Dimroth rearrangement. In the case of 1<i>H</i>-benzo[<i>f</i>]chromene-2-carbaldehydes, the corresponding Knoevenagel adducts were isolated.</p>","PeriodicalId":9770,"journal":{"name":"Chemistry of Heterocyclic Compounds","volume":"69 1","pages":""},"PeriodicalIF":1.5,"publicationDate":"2024-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141255441","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}