Synthesis and trypanocidal activity of substituted 2, 4-diarylquinoline derivatives
- Oluwafemi, Kola A, Phunguphungu, Siyolise, Gqunu, Sinalo, Isaacs, Michelle, Hoppe, Heinrich C, Klein, Rosalyn, Kaye, Perry T
- Authors: Oluwafemi, Kola A , Phunguphungu, Siyolise , Gqunu, Sinalo , Isaacs, Michelle , Hoppe, Heinrich C , Klein, Rosalyn , Kaye, Perry T
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/477683 , vital:78111 , xlink:href="https://doi.org/10.24820/ark.5550190.p011.499"
- Description: A small library of nine, novel 2, 4-diarylquinoline derivatives has been prepared in high yield via convenient one-or two-step routes from a series of substituted 2-aminobenzophenones. None of the products exhibited toxicity at 20 μM against human cervix adenocarcinoma (HeLa) cells, while many of them exhibited encouraging trypanocidal activity against T. brucei brucei (a parasite responsible for African cattle trypanosomiasis)-some with IC50 values in the range 2.8–6.2 μM.
- Full Text:
- Authors: Oluwafemi, Kola A , Phunguphungu, Siyolise , Gqunu, Sinalo , Isaacs, Michelle , Hoppe, Heinrich C , Klein, Rosalyn , Kaye, Perry T
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/477683 , vital:78111 , xlink:href="https://doi.org/10.24820/ark.5550190.p011.499"
- Description: A small library of nine, novel 2, 4-diarylquinoline derivatives has been prepared in high yield via convenient one-or two-step routes from a series of substituted 2-aminobenzophenones. None of the products exhibited toxicity at 20 μM against human cervix adenocarcinoma (HeLa) cells, while many of them exhibited encouraging trypanocidal activity against T. brucei brucei (a parasite responsible for African cattle trypanosomiasis)-some with IC50 values in the range 2.8–6.2 μM.
- Full Text:
Rational design and regioselective synthesis of conformationally restricted furan-derived ligands as potential anti-malarial agents
- Mutorwa, Marius K, Nokalipa, Iviwe, Tanner, Delia C, Blatch, Gregory L, Lobb, Kevin A, Klein, Rosalyn, Kaye, Perry T
- Authors: Mutorwa, Marius K , Nokalipa, Iviwe , Tanner, Delia C , Blatch, Gregory L , Lobb, Kevin A , Klein, Rosalyn , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447170 , vital:74589 , xlink:href="https://doi.org/10.24820/ark.5550190.p011.281"
- Description: Substituted 3-furanomethyl phosphate esters and their corresponding phosphoric acids have been prepared as conformationally restricted analogues of DOXP, the natural substrate for Plasmodium falciparum 1-deoxyD-xylulose-5-phosphate reductoisomerase (PfDXR), and fosmidomycin, an established inhibitor. Saturation Transfer Difference (STD) NMR analysis and in silico docking data suggest the potential of such compounds as PfDXR inhibitors.
- Full Text:
- Authors: Mutorwa, Marius K , Nokalipa, Iviwe , Tanner, Delia C , Blatch, Gregory L , Lobb, Kevin A , Klein, Rosalyn , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/447170 , vital:74589 , xlink:href="https://doi.org/10.24820/ark.5550190.p011.281"
- Description: Substituted 3-furanomethyl phosphate esters and their corresponding phosphoric acids have been prepared as conformationally restricted analogues of DOXP, the natural substrate for Plasmodium falciparum 1-deoxyD-xylulose-5-phosphate reductoisomerase (PfDXR), and fosmidomycin, an established inhibitor. Saturation Transfer Difference (STD) NMR analysis and in silico docking data suggest the potential of such compounds as PfDXR inhibitors.
- Full Text:
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