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Anticancer activity of structural hybrids of various 5/6-memberedheterocycles with pyrazolobenzothiazine 5,5-dioxide

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dc.contributor.author Aslam, Sana
dc.contributor.author Xi, Yun
dc.contributor.author Ahmad, Matloob
dc.contributor.author Mansha, Asim
dc.contributor.author Farooq, Tahir
dc.contributor.author Zheng, Zongheng
dc.contributor.author Ahmad Saddique, Furqan
dc.contributor.author Wang, Fang
dc.contributor.author Fu, Liwu
dc.date.accessioned 2022-10-07T10:54:01Z
dc.date.available 2022-10-07T10:54:01Z
dc.date.issued 2020-05-04
dc.identifier.citation Aslam, S., Xi, Y., Ahmad, M., Mansha, A., Farooq, T., Zheng, Z., ... & Fu, L. (2020). Anticancer activity of structural hybrids of various 5/6-membered-heterocycles with pyrazolobenzothiazine 5, 5-dioxide. PAKISTAN JOURNAL OF PHARMACEUTICAL SCIENCES, 33(3), 1239-1243. en_US
dc.identifier.issn 1011-601X
dc.identifier.uri http://142.54.178.187:9060/xmlui/handle/123456789/12814
dc.description.abstract Thiophene, furan, coumarin and pyrazolobenzothiazine are well familiar for their biological activities. In this research, pyrazolobenzothiazine ring system is hybridized with various S, N & O-containing heterocycles and the resulting compounds were screened for their anticancer activity against six different cancer cell lines i.e., KB (human oral carcinoma cells), MCF-7(human breast carcinoma cells), A549 (human alveolar adenocarcinoma cells), Hep-G2 (liver carcinoma cells), SGC-7901(human gastric carcinoma cells) and S1 (human colon carcinoma cells) using MTT assay. Most of the compounds exhibited good activity against KB, S1 and A549 cancer cell lines. 5k and 5p appeared as potent inhibitors of KB cell line with IC50 values 2.78 and 4.39 μM respectively, 5q was a potent inhibitor of MCF-7 (IC50 value = 13.64 μM) and 5j an excellent inhibitor of A549 cell line having IC50value of 1.03 μM. 5p and 5q were inhibitors of S1 cell line (IC50 values of 8.29 μM and 7.69 μM respectively), whereas, 5o and 5q as inhibitors of Hep-G2 cell line were discovered. A number of compounds show activity exceeding that of 5-fluoruracil in different cell assays. The most potently active compounds, 5j, 5p and 5q, exhibited selectivity in targeting cancerous cells as compared to normal human PBM cells while, 5k and 5o displayed significant toxicity in normal cells. en_US
dc.language.iso en en_US
dc.publisher Karachi:Pakistan Journal of Pharmaceutical Sciences, university of Karachi. en_US
dc.subject Pyrazolobenzothiazine en_US
dc.subject anti-cancer activity en_US
dc.subject cytotoxicity en_US
dc.subject selective inhbition en_US
dc.title Anticancer activity of structural hybrids of various 5/6-memberedheterocycles with pyrazolobenzothiazine 5,5-dioxide en_US
dc.type Article en_US


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