Cinnamoyl-Oxaborole Amides: Synthesis and Their in Vitro Biological Activity.
- Gumbo, Maureen, Beteck, Richard M, Mandizvo, Tawanda, Seldon, Ronnett, Warner, Digby F, Hoppe, Heinrich C, Isaacs, Michelle, Laming, Dustin, Tam, Christina C, Cheng, Luisa W, Liu, Nicole, Land, Kirkwood, Khanye, Setshaba D
- Authors: Gumbo, Maureen , Beteck, Richard M , Mandizvo, Tawanda , Seldon, Ronnett , Warner, Digby F , Hoppe, Heinrich C , Isaacs, Michelle , Laming, Dustin , Tam, Christina C , Cheng, Luisa W , Liu, Nicole , Land, Kirkwood , Khanye, Setshaba D
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/122879 , vital:35362 , https://doi.org/10.3390/molecules23082038
- Description: Due to the increased interest in their application in the treatment of infectious diseases, boron-containing compounds have received a significant coverage in the literature. Herein, a small set of novel cinnamoly-oxaborole amides were synthesized and screened against nagana Trypanosoma brucei brucei for antitrypanosomal activity. Compound 5g emerged as a new hit with an in vitro IC50 value of 0.086 μM against T. b. brucei without obvious inhibitory activity against HeLa cell lines. The same series was also screened against other human pathogens, including Mycobacterium tuberculosis, the causative agent of tuberculosis (TB), for which moderate to weak activity (10 to >125 μM) was observed. Similarly, these compounds exhibited moderate activity against the human protozoal pathogen Trichomonas vaginalis with no observed effect on common microbiome bacterial species. The cross-species inhibitory activity presents the possibility of these compounds serving as broad-spectrum antibiotics for these prevalent three human pathogens.
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- Authors: Gumbo, Maureen , Beteck, Richard M , Mandizvo, Tawanda , Seldon, Ronnett , Warner, Digby F , Hoppe, Heinrich C , Isaacs, Michelle , Laming, Dustin , Tam, Christina C , Cheng, Luisa W , Liu, Nicole , Land, Kirkwood , Khanye, Setshaba D
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/122879 , vital:35362 , https://doi.org/10.3390/molecules23082038
- Description: Due to the increased interest in their application in the treatment of infectious diseases, boron-containing compounds have received a significant coverage in the literature. Herein, a small set of novel cinnamoly-oxaborole amides were synthesized and screened against nagana Trypanosoma brucei brucei for antitrypanosomal activity. Compound 5g emerged as a new hit with an in vitro IC50 value of 0.086 μM against T. b. brucei without obvious inhibitory activity against HeLa cell lines. The same series was also screened against other human pathogens, including Mycobacterium tuberculosis, the causative agent of tuberculosis (TB), for which moderate to weak activity (10 to >125 μM) was observed. Similarly, these compounds exhibited moderate activity against the human protozoal pathogen Trichomonas vaginalis with no observed effect on common microbiome bacterial species. The cross-species inhibitory activity presents the possibility of these compounds serving as broad-spectrum antibiotics for these prevalent three human pathogens.
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Happiness: a business model
- Authors: Cullen, Margaret
- Subjects: Happiness , f-sa
- Language: English
- Type: text , Lectures
- Identifier: http://hdl.handle.net/10948/20956 , vital:29422
- Description: The concept of happiness might appear elusive. It has been extensively analysed by philosophers and historians, who agree that the concept of happiness in antiquity centered on good luck and fortune. Something beyond human agency and therefore controlled by the Gods (McMahon, 2006).Today, happiness is viewed as something over which you can have control and something that can be pursued (Oishi, 2012).
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- Authors: Cullen, Margaret
- Subjects: Happiness , f-sa
- Language: English
- Type: text , Lectures
- Identifier: http://hdl.handle.net/10948/20956 , vital:29422
- Description: The concept of happiness might appear elusive. It has been extensively analysed by philosophers and historians, who agree that the concept of happiness in antiquity centered on good luck and fortune. Something beyond human agency and therefore controlled by the Gods (McMahon, 2006).Today, happiness is viewed as something over which you can have control and something that can be pursued (Oishi, 2012).
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Novobiocin–ferrocene conjugates possessing anticancer and antiplasmodial activity independent of HSP90 inhibition.
- Mbaba, Mziyanda, de la Mare, Jo-Anne, Sterrenberg, Jason N, Kajewole, Deborah, Maharaj, Shantal, Edkins, Adrienne L, Isaacs, Michelle, Hoppe, Heinrich C, Khanye, Setshaba D
- Authors: Mbaba, Mziyanda , de la Mare, Jo-Anne , Sterrenberg, Jason N , Kajewole, Deborah , Maharaj, Shantal , Edkins, Adrienne L , Isaacs, Michelle , Hoppe, Heinrich C , Khanye, Setshaba D
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/122858 , vital:35359 , https://doi.org/10.1007/s00775-018-1634-9
- Description: A series of tailored novobiocin–ferrocene conjugates was prepared in moderate yields and investigated for in vitro anticancer and antiplasmodial activity against the MDA-MB-231 breast cancer line and Plasmodium falciparum 3D7 strain, respectively. While the target compounds displayed moderate anticancer activity against the breast cancer cell line with IC50 values in the mid-micromolar range, compounds 10a–c displayed promising antiplasmodial activity as low as 0.889 µM. Furthermore, the most promising compounds were tested for inhibitory effects against a postulated target, heat shock protein 90 (Hsp90).
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- Authors: Mbaba, Mziyanda , de la Mare, Jo-Anne , Sterrenberg, Jason N , Kajewole, Deborah , Maharaj, Shantal , Edkins, Adrienne L , Isaacs, Michelle , Hoppe, Heinrich C , Khanye, Setshaba D
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/122858 , vital:35359 , https://doi.org/10.1007/s00775-018-1634-9
- Description: A series of tailored novobiocin–ferrocene conjugates was prepared in moderate yields and investigated for in vitro anticancer and antiplasmodial activity against the MDA-MB-231 breast cancer line and Plasmodium falciparum 3D7 strain, respectively. While the target compounds displayed moderate anticancer activity against the breast cancer cell line with IC50 values in the mid-micromolar range, compounds 10a–c displayed promising antiplasmodial activity as low as 0.889 µM. Furthermore, the most promising compounds were tested for inhibitory effects against a postulated target, heat shock protein 90 (Hsp90).
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The Plastic University: Knowledge, Disciplines and Decolonial 'Circulations'
- Authors: Keet, Andre
- Subjects: Critical pedagogy , Transformative learning , f-sa
- Language: English
- Type: text , Lectures
- Identifier: http://hdl.handle.net/10948/21077 , vital:29436
- Description: The university is as plastic as the social figure of ‘Mandela’ after whom it is named. It is as plastic as the globe and its humanity in whose name it exists. And, it is as plastic as the human subject that is ‘perpetually called on to reconfigure itself in relation to the artefacts of the age’, as Mbembe2 argues in Critique of Black Reason. The very nature of addressing, of writing … of inaugurating … oneself, through an address is an act of reconfiguration, of responding to an artefact of the university and the professoriate. It is, when all is said and done, a performance, a performative act: declaring so and so a professor of this or that status, authorizing ‘it’ to utter something with some kind of formative force.
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- Authors: Keet, Andre
- Subjects: Critical pedagogy , Transformative learning , f-sa
- Language: English
- Type: text , Lectures
- Identifier: http://hdl.handle.net/10948/21077 , vital:29436
- Description: The university is as plastic as the social figure of ‘Mandela’ after whom it is named. It is as plastic as the globe and its humanity in whose name it exists. And, it is as plastic as the human subject that is ‘perpetually called on to reconfigure itself in relation to the artefacts of the age’, as Mbembe2 argues in Critique of Black Reason. The very nature of addressing, of writing … of inaugurating … oneself, through an address is an act of reconfiguration, of responding to an artefact of the university and the professoriate. It is, when all is said and done, a performance, a performative act: declaring so and so a professor of this or that status, authorizing ‘it’ to utter something with some kind of formative force.
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