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Aryl sulfonate based anticancer alkylating agents

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dc.contributor.author Sheikh, Hamdullah Khadim
dc.contributor.author Tanzila Arshad
dc.contributor.author Ghazala Kanwal
dc.date.accessioned 2023-01-19T04:36:05Z
dc.date.available 2023-01-19T04:36:05Z
dc.date.issued 2018-05-16
dc.identifier.citation Sheikh, H. K., Arshad, T., & Kanwal, G. (2018). Aryl sulfonate based anticancer alkylating agents. Pakistan Journal of Pharmaceutical Sciences, 31. en_US
dc.identifier.issn 1011-601X
dc.identifier.uri http://142.54.178.187:9060/xmlui/handle/123456789/16077
dc.description.abstract This research work revolves around synthesis of antineoplastic alkylating sulfonate esters with dual alkylating sites for crosslinking of the DNA strands. These molecules were evaluated as potential antineoplastic cross linking alkylating agents by reaction with the nucleoside of Guanine DNA nucleobase at both ends of the synthesized molecule. Synthesis of the alkylating molecules and the crosslinking with the guanosine nucleoside was monitored by MALDITOF mass spectroscopy. The synthesized molecule’s crosslinking or adduct forming rate with the nucleoside was compared with that of 1,4 butane disulfonate (busulfan), in form of time taken for the appearance of [M+H]+ . It was found that aryl sulfonate leaving group was causing higher rate of nucleophilic attack by the Lewis basic site of the nucleobase. Furthermore, the rate was also found to be a function of electron withdrawing or donating nature of the substituent on the aryl ring. Compound with strong electron withdrawing substituent on the para position of the ring reacted fastest. Hence, new alkylating agents were synthesized with optimized or desired reactivity. en_US
dc.language.iso en en_US
dc.publisher Karachi: Faculty of Pharmacy & Pharmaceutical Sciences University of Karachi en_US
dc.subject Organic synthesis en_US
dc.subject alkylation en_US
dc.subject MALDI-MS en_US
dc.subject antineoplastic en_US
dc.subject busulphan en_US
dc.title Aryl sulfonate based anticancer alkylating agents en_US
dc.type Article en_US


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