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- 01HRYKBMP36E1W3RFQQSZ3J2T0 classification C3.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 date "2022".
- 01HRYKBMP36E1W3RFQQSZ3J2T0 language "eng".
- 01HRYKBMP36E1W3RFQQSZ3J2T0 type conference.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 hasPart 01HRYKRXD6C010MHKYCZCF3J39.pdf.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 subject "Medicine and Health Sciences".
- 01HRYKBMP36E1W3RFQQSZ3J2T0 presentedAt urn:uuid:e3a443a9-7215-4d59-9571-58bc148a3592.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 abstract "Cancer remains, to this day, one of the leading causes of death worldwide. According to the World Health Organisation, nearly 10 million deaths were attributed to some type of cancer in 2020. Therefore, new therapeutic treatments in oncology are still highly desirable. Curcumin is a natural product, extracted from the rhizomes of the Curcuma longa plant. It has been used as a food additive predominantly in the South Asian cuisine for centuries, and it exerts a broad range of biological activities (antioxidant, anti-inflammatory, antimicrobial, anticancer…). With respect to its contribution to the field of cancer research, curcumin has shown to inhibit cancer cell proliferation, proving itself a potential drug candidate for further development. However, its low bioavailability, low stability and aspecific activity cannot be disregarded. Especially the aspecific activity is a matter of concern, as it plays a role in the pan-assay interference (“PAINS”) properties exhibited by curcumin. Covalent and aspecific binding to target proteins, redox cycling resulting in peroxide formation, metal chelation and fluorescence interference are all examples that can lead to a false positive readout in assays. Profound structural modifications of the curcumin scaffold are thus necessary to progress towards a more suitable drug candidate. Previous research in our group has led to the discovery of two unprecedented thiazepane-based derivatives with promising anticancer activity, considerably moving away from the traditional curcumin structure. The introduction of three-dimensionality to the molecule improved properties related to drug-likeness, such as solubility and bioavailability. In addition, PAINS-activity that can be attributed to the structural properties of the molecule could, in this way, be circumvented as well. In that regard, we recently developed a small library of functionalized benzothiazepane systems to explore their biological activity in the context of cancer cell cytotoxicity. In this presentation, we will discuss the chemistry developed to allow the synthesis of these new molecules, their biological properties in terms of cytotoxicity against a panel of cancer cells, and some physicochemical properties, followed by concluding SAR insights and prospects for future research.".
- 01HRYKBMP36E1W3RFQQSZ3J2T0 author CAEEDD34-2D6C-11E4-A9C7-B2F1B4D1D7B1.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 author F4B233EA-F0ED-11E1-A9DE-61C894A0A6B4.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 author F639DE16-F0ED-11E1-A9DE-61C894A0A6B4.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 author F82E0150-8460-11E7-A72F-CA7AAD28A064.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 author urn:uuid:228b3c89-95b6-4987-ae0f-1aa08db29e7a.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 dateCreated "2024-03-14T13:45:21Z".
- 01HRYKBMP36E1W3RFQQSZ3J2T0 dateModified "2024-12-12T20:15:33Z".
- 01HRYKBMP36E1W3RFQQSZ3J2T0 name "The natural product curcumin as a source of inspiration for the development of novel benzothiazepane-based cancer cell cytotoxic agents".
- 01HRYKBMP36E1W3RFQQSZ3J2T0 sameAs LU-01HRYKBMP36E1W3RFQQSZ3J2T0.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 sourceOrganization urn:uuid:1cbf5ca9-3ea4-4751-b6d0-67541375884b.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 sourceOrganization urn:uuid:92627c6d-bc09-43e8-9803-38d77b8ee231.
- 01HRYKBMP36E1W3RFQQSZ3J2T0 type C3.