In the present work, we have systematically studied the dark and photoinduced cytotoxicity of a series of chlorophyll a derivatives (a sampling of 36 compounds, the quantitative measure of toxicity is HeLa cell survival and IC 50 value) in experiments in vitro. It has been shown that chlorins without an exocycle, such as chlorin e 6 , its 15,17-dimethyl ether and 13-amide derivatives, regardless of the substituent at the 13-amide nitrogen atom, as well as substituents in positions 3, 15 and 17, as a rule, have the highest cytotoxicity (IC 50 ( dark ) < 10 µM). It has been established that the IC 50 value during the dark exposure is more than 10 µM for the most part of phorbin pounds with different dark toxicity showed that substances with both high and low dark toxicity have high IC 50(dark) /IC 50(photo) values, so the effectiveness of the photosensitizer is not unambiguously associated with its low dark toxicity.
{"title":"Dark and Photoinduced Cytotoxicity of Chlorophyll a Derivatives and Their Analogues towards HeLa Cells: Some Structure - Activity Relationships","authors":"Y. Pylina, I. Khudyaeva, D. V. Belykh","doi":"10.6060/mhc224176b","DOIUrl":"https://doi.org/10.6060/mhc224176b","url":null,"abstract":"In the present work, we have systematically studied the dark and photoinduced cytotoxicity of a series of chlorophyll a derivatives (a sampling of 36 compounds, the quantitative measure of toxicity is HeLa cell survival and IC 50 value) in experiments in vitro. It has been shown that chlorins without an exocycle, such as chlorin e 6 , its 15,17-dimethyl ether and 13-amide derivatives, regardless of the substituent at the 13-amide nitrogen atom, as well as substituents in positions 3, 15 and 17, as a rule, have the highest cytotoxicity (IC 50 ( dark ) < 10 µM). It has been established that the IC 50 value during the dark exposure is more than 10 µM for the most part of phorbin pounds with different dark toxicity showed that substances with both high and low dark toxicity have high IC 50(dark) /IC 50(photo) values, so the effectiveness of the photosensitizer is not unambiguously associated with its low dark toxicity.","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71167891","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}
D. V. Beigulenko, N. Shepeta, K. Kochetkov, S. Gelperina
Studies of various aspects of the action of vitamin B 12 bring interesting, often unexpected, results and open up new prospects for their practical application. The review focuses on recent advances in the use of natural cobalamins and their synthetic analogues in medical practice as vectors for targeted drug delivery to tumors. Particular attention is paid to the rationale for the use of corrinoids in this area in terms of their biodistribution and metabolism in the hu-man body. The most common in nature cobalamins and a number of the most important synthetic derivatives of vitamin B 12 , the absorption and distribution of cobalamins, the main functions of vitamin B 12 in the cell, general ap-proaches to bioorthogonal (i.e., preserving the biological functions of the molecule) modification, as well as consid-eration of sites in the structure of this compound, which are most suitable for conjugation, are successively discussed. The use of corrinoids for the diagnosis of tumors and drug delivery is considered separately. Examples of the synthesis of conjugates of cobalamins and various low molecular weight drugs, as well as proteins and oligonucleotides and targeted transport of the resulting compounds in tumors are analyzed. In conclusion, examples of the use of cobalamins as promising vectors for various colloidal delivery systems, including micro and nanoparticles, are given. The obtained results testify to the prospects of this direction. Of particular importance to the authors is the develop-ment of cobalamin-vectored drug delivery vehicles for chemotherapy of tumors, for which an increased expression of vitamin B 12 transport proteins is observed.
{"title":"Vitamin B12 as a Vector for the Transport of Drugs to the Tumor","authors":"D. V. Beigulenko, N. Shepeta, K. Kochetkov, S. Gelperina","doi":"10.6060/mhc224244k","DOIUrl":"https://doi.org/10.6060/mhc224244k","url":null,"abstract":"Studies of various aspects of the action of vitamin B 12 bring interesting, often unexpected, results and open up new prospects for their practical application. The review focuses on recent advances in the use of natural cobalamins and their synthetic analogues in medical practice as vectors for targeted drug delivery to tumors. Particular attention is paid to the rationale for the use of corrinoids in this area in terms of their biodistribution and metabolism in the hu-man body. The most common in nature cobalamins and a number of the most important synthetic derivatives of vitamin B 12 , the absorption and distribution of cobalamins, the main functions of vitamin B 12 in the cell, general ap-proaches to bioorthogonal (i.e., preserving the biological functions of the molecule) modification, as well as consid-eration of sites in the structure of this compound, which are most suitable for conjugation, are successively discussed. The use of corrinoids for the diagnosis of tumors and drug delivery is considered separately. Examples of the synthesis of conjugates of cobalamins and various low molecular weight drugs, as well as proteins and oligonucleotides and targeted transport of the resulting compounds in tumors are analyzed. In conclusion, examples of the use of cobalamins as promising vectors for various colloidal delivery systems, including micro and nanoparticles, are given. The obtained results testify to the prospects of this direction. Of particular importance to the authors is the develop-ment of cobalamin-vectored drug delivery vehicles for chemotherapy of tumors, for which an increased expression of vitamin B 12 transport proteins is observed.","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71168820","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}
Mahmoud Hamdoush, Sergey Sigunov, I. Skvortsov, Ekaterina N Tarakanova, P. Stuzhin
{"title":"Electrochemical study of the lanthanide complexes of tetra(1,2,5-thiadiazolo)porphyrazine, [TSDPzLn(acac)] (Ln = SmIII, EuIII, DyIII, ErIII, LuIII)","authors":"Mahmoud Hamdoush, Sergey Sigunov, I. Skvortsov, Ekaterina N Tarakanova, P. Stuzhin","doi":"10.6060/mhc224831s","DOIUrl":"https://doi.org/10.6060/mhc224831s","url":null,"abstract":"","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71169169","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}
A. S. Chuprin, A. Vologzhanina, A. Loktev, M. G. Bugaenko, Y. Voloshin, V. Buznik, A. Dedov
{"title":"Preparation of a Hybrid Сeramic-Based Material with Immobilized Dicarboxyl-Terminated Ruthenium(II) Clathrochelate and Its Catalytic Activity in Methane Oxidative Conversion","authors":"A. S. Chuprin, A. Vologzhanina, A. Loktev, M. G. Bugaenko, Y. Voloshin, V. Buznik, A. Dedov","doi":"10.6060/mhc224374z","DOIUrl":"https://doi.org/10.6060/mhc224374z","url":null,"abstract":"","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"9 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71169431","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}
M. Sathiyaseelan, K. Sathishkumar, A. Nepolraj, J. A. Malik, Vasyl Shupeniukd
{"title":"Design, Synthesis and Molecular Docking Studies of Indolo[2,3-a]Acridinol Derivatives","authors":"M. Sathiyaseelan, K. Sathishkumar, A. Nepolraj, J. A. Malik, Vasyl Shupeniukd","doi":"10.6060/mhc224206n","DOIUrl":"https://doi.org/10.6060/mhc224206n","url":null,"abstract":"","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71168428","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}
{"title":"Synthesis of a New N-Substituted Carbazolocyanines with Absorption in the Near IR Region","authors":"M. Belousov, A. Kosov, N. Borisova, T. Dubinina","doi":"10.6060/mhc224298d","DOIUrl":"https://doi.org/10.6060/mhc224298d","url":null,"abstract":"","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71168645","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}
N. V. Tverdova, N. Giricheva, V. Maizlish, N. Galanin, G. V. Girichev
The conformational properties and structure of the conformers of 4-(4-tritylphenoxy)phthalonitrile (C 33 H 22 N 2 O), acting as a precursor for the synthesis of tritylphenoxy substituted phthalocyanines, were investigated by DFT method. The conformational analysis of the C 33 H 22 N 2 O molecule indicates the possibility of formation of conformers of substituted phthalocyanines with different orientations of 4-tritylphenoxy substituents, including those with a combination of cis- and trans- positions within one complex.
{"title":"From Сonformational Properties of 4-(4-Tritylphenoxy)phthalonitrile Precursor to Conformational Properties of Substituted Phthalocyanines","authors":"N. V. Tverdova, N. Giricheva, V. Maizlish, N. Galanin, G. V. Girichev","doi":"10.6060/mhc214086g","DOIUrl":"https://doi.org/10.6060/mhc214086g","url":null,"abstract":"The conformational properties and structure of the conformers of 4-(4-tritylphenoxy)phthalonitrile (C 33 H 22 N 2 O), acting as a precursor for the synthesis of tritylphenoxy substituted phthalocyanines, were investigated by DFT method. The conformational analysis of the C 33 H 22 N 2 O molecule indicates the possibility of formation of conformers of substituted phthalocyanines with different orientations of 4-tritylphenoxy substituents, including those with a combination of cis- and trans- positions within one complex.","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71167959","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}
D. V. Belykh, E. I. Pushkareva, G. V. Kutaeva, N. D. Belykh, D. Serova, I. Velegzhaninov
{"title":"Synthesis, dark and photoinduced cytotoxicity of 1-alkoxy-2-iodoethyl derivatives of chlorophyll a","authors":"D. V. Belykh, E. I. Pushkareva, G. V. Kutaeva, N. D. Belykh, D. Serova, I. Velegzhaninov","doi":"10.6060/mhc224280b","DOIUrl":"https://doi.org/10.6060/mhc224280b","url":null,"abstract":"","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71168521","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}
S. V. Zvezdina, N. Chizhova, N. Mamardashvili, O. Koifman
{"title":"Effect of halogenation of ortho-positions of tetraphenylporphyrin and its Cd(II) complex on their complexing ability towards d-metal salts in dimethylformamide","authors":"S. V. Zvezdina, N. Chizhova, N. Mamardashvili, O. Koifman","doi":"10.6060/mhc224315m","DOIUrl":"https://doi.org/10.6060/mhc224315m","url":null,"abstract":"","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71168698","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}
G. S. Zabrodina, M. A. Katkova, R. Rumyantcev, G. Zhigulin, S. Ketkov
{"title":"The First Ate Complex of Copper(II) 5-Chlorosalicylhydroximate Metallacrown with Outer-Sphere Nickel(II) Cation","authors":"G. S. Zabrodina, M. A. Katkova, R. Rumyantcev, G. Zhigulin, S. Ketkov","doi":"10.6060/mhc224316z","DOIUrl":"https://doi.org/10.6060/mhc224316z","url":null,"abstract":"","PeriodicalId":18090,"journal":{"name":"Macroheterocycles","volume":"1 1","pages":""},"PeriodicalIF":1.4,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71168976","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}
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