Abstract
Cancer is the world's second-largest cause of mortality and one of the biggest global health concerns. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective, as well as less toxic treatment methods for cancer, is at the focus of current studies. Thiophene and its derivatives have surged as an influential scaffold, which, because of their appreciable diversity in biological activities, has drawn the concerned interest of the researchers in the field of medicinal chemistry. By the affluent introduction of its derivatives, which have antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, the adaptability of the thiophene moiety has been displayed. The nature and positioning of the substitutions significantly impacted thiophene moiety activity. This decent array in the living response account about this moiety has picked plentiful researcher’s consideration to inquire about it to its peculiar potential across certain activities. In the field of cancer therapy against different cancer cells, the structure-activity relationship for each of the derivatives showed an excellent understanding of thiophene moiety. Information from the various articles revealed the key role of thiophene moiety and its derivatives to develop the vital lead compound. The essential anticancer mechanisms identified include inhibition of the topoisomerase, inhibition of tyrosine kinase, tubulin interaction and apoptosis induction through the activation of reactive oxygen species. This review is an endeavor to promote the anticancer potential of the derivatives, whether having thiophene or condensed thiophene as a core moiety or as a substituent that can lead in the future to synthesize varieties of chemotherapeutic entities in the field of cancer treatment.
Keywords: Thiophene, structure-activity relationship, anticancer activity, cell lines, antimicrobial, anti-inflammatory, antioxidant
Graphical Abstract
[http://dx.doi.org/10.3322/caac.21492] [PMID: 30207593]
[http://dx.doi.org/10.1002/ijc.29210] [PMID: 25220842]
[http://dx.doi.org/10.1126/science.1126758] [PMID: 16728627]
[http://dx.doi.org/10.1002/jhet.3249]
[PMID: 29256900]
[PMID: 8382551]
[http://dx.doi.org/10.1186/s13065-019-0569-8] [PMID: 31384802]
[http://dx.doi.org/10.1016/j.ejmech.2012.10.007] [PMID: 23149297]
[http://dx.doi.org/10.1016/j.ejmech.2006.11.007] [PMID: 17189665]
[http://dx.doi.org/10.1002/jhet.5570250559]
[http://dx.doi.org/10.1002/slct.201800613]
[http://dx.doi.org/10.1089/dna.2017.3962] [PMID: 29215922]
[http://dx.doi.org/10.1016/j.bioorg.2016.09.001] [PMID: 27616159]
[http://dx.doi.org/10.3390/molecules24010192] [PMID: 30621360]
[http://dx.doi.org/10.3390/ijms17091499] [PMID: 27618013]
[http://dx.doi.org/10.1007/s00044-016-1703-y]
[http://dx.doi.org/10.1016/j.ejmech.2015.09.036] [PMID: 26454648]
[http://dx.doi.org/10.2478/acph-2014-0035] [PMID: 25531783]
[http://dx.doi.org/10.2478/v10007-012-0017-y] [PMID: 22750820]
[http://dx.doi.org/10.1016/j.bmc.2005.12.004] [PMID: 16412644]
[http://dx.doi.org/10.1016/S0968-0896(02)00654-5] [PMID: 12628643]
[http://dx.doi.org/10.1016/j.molstruc.2016.08.056]
[http://dx.doi.org/10.1016/j.biopha.2016.09.026]
[http://dx.doi.org/10.1016/j.bmc.2013.12.030] [PMID: 24398384]
[http://dx.doi.org/10.4236/ijoc.2016.62009]
[http://dx.doi.org/10.1016/j.jscs.2012.06.004]
[http://dx.doi.org/10.1016/j.bmcl.2015.11.010] [PMID: 26602281]
[http://dx.doi.org/10.1515/acph-2016-0016] [PMID: 27279061]
[http://dx.doi.org/10.1016/j.bmcl.2016.08.013] [PMID: 27546293]
[http://dx.doi.org/10.1016/j.ejmech.2015.08.053] [PMID: 26363869]
[http://dx.doi.org/10.1016/j.bmc.2015.04.037] [PMID: 25975637]
[PMID: 25265819]
[http://dx.doi.org/10.1055/s-0033-1337928] [PMID: 23529721]
[http://dx.doi.org/10.1016/j.bmcl.2010.11.083] [PMID: 21146985]
[http://dx.doi.org/10.3390/molecules16010052] [PMID: 21187817]
[http://dx.doi.org/10.1016/j.bmc.2008.04.026] [PMID: 18440234]
[http://dx.doi.org/10.1016/j.bmc.2008.05.034] [PMID: 18524604]
[http://dx.doi.org/10.1016/j.bmcl.2007.01.065] [PMID: 17306531]
[http://dx.doi.org/10.3390/12030497] [PMID: 17851406]
[http://dx.doi.org/10.1016/j.tet.2006.07.095]
[http://dx.doi.org/10.1016/S0960-894X(01)00436-X] [PMID: 11527727]
[http://dx.doi.org/10.1016/S0960-894X(99)00375-3] [PMID: 10465561]
[http://dx.doi.org/10.1016/j.bmc.2019.07.042] [PMID: 31416740]
[http://dx.doi.org/10.1021/acsomega.9b00554] [PMID: 31459975]
[http://dx.doi.org/10.1080/10717544.2020.1716879] [PMID: 31984809]
[http://dx.doi.org/10.3390/molecules25010064] [PMID: 31878135]
[http://dx.doi.org/10.1016/j.ejmech.2010.09.038] [PMID: 20933308]
[http://dx.doi.org/10.1016/j.bmc.2010.05.068] [PMID: 20579891]
[http://dx.doi.org/10.1039/c3md00130j] [PMID: 23956835]
[http://dx.doi.org/10.1016/j.bmc.2010.04.046] [PMID: 20466555]
[http://dx.doi.org/10.1016/j.bmc.2004.02.007] [PMID: 15080924]
[http://dx.doi.org/10.1515/acph-2017-0004] [PMID: 28231053]
[http://dx.doi.org/10.1016/j.ejmech.2016.07.022] [PMID: 27474924]
[http://dx.doi.org/10.1007/s00044-014-1273-9]
[http://dx.doi.org/10.1007/s00044-016-1692-x]
[http://dx.doi.org/10.1021/jm400043d] [PMID: 23445496]
[http://dx.doi.org/10.7598/cst2012.175]
[http://dx.doi.org/10.1016/j.bmc.2006.06.046] [PMID: 16837202]
[http://dx.doi.org/10.1016/j.ejmech.2010.02.032] [PMID: 20219270]
[http://dx.doi.org/10.1016/S0960-894X(99)00088-8] [PMID: 10206538]
[http://dx.doi.org/10.1002/jhet.3629]
[http://dx.doi.org/10.1016/j.bmcl.2009.01.080] [PMID: 19208477]
[http://dx.doi.org/10.1016/S0968-0896(98)00241-7] [PMID: 10428370]
[http://dx.doi.org/10.1007/s00706-015-1542-4]
[http://dx.doi.org/10.1016/j.ejmech.2016.09.068] [PMID: 27718470]
[http://dx.doi.org/10.1016/j.bmc.2016.05.041] [PMID: 27283788]
[PMID: 25015456]