Willem A L van Otterlo
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Explore the profile of Willem A L van Otterlo including associated specialties, affiliations and a list of published articles.
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Recent Articles
1.
Panayides J, Riley D, Hasenmaile F, van Otterlo W
RSC Med Chem
. 2024 Oct;
15(10):3286-3344.
PMID: 39430101
This review aims to highlight the role of silicon in drug discovery. Silicon and carbon are often regarded as being similar with silicon located directly beneath carbon in the same...
2.
Ingels A, Scott R, Hooper A, van der Westhuyzen A, Wagh S, de Meester J, et al.
Sci Rep
. 2024 Jun;
14(1):14674.
PMID: 38918539
Sphaeropsidins are iso-pimarane diterpenes produced by phytopathogenic fungi that display promising anticancer activities. Sphaeropsidin A, in particular, has been shown to counteract regulatory volume increase, a process used by cancer...
3.
Wagh S, Berthold D, Majeed I, Lewis L, Schilter D, Mertens B, et al.
ChemMedChem
. 2024 Jun;
19(18):e202400288.
PMID: 38895989
We recently discovered that sphaeropsidin A (SphA), a fungal metabolite from Diplodia cupressi, overcomes apoptosis resistance in cancer cells by inducing cellular shrinkage by impairing regulatory volume increase. Previously, we...
4.
van der Westhuyzen A, Ashraf N, Conradie D, Loots L, Kaschula C, Pelly S, et al.
J Med Chem
. 2024 Jun;
67(12):9950-9975.
PMID: 38865195
To improve their aqueous solubility characteristics, water-solubilizing groups were added to some antiproliferative, rigidin-inspired 7-deazahypoxanthine frameworks after molecular modeling seemed to indicate that structural modifications on the C7 and/or C8...
5.
Gross D, van Otterlo W, Trapp O, Berthold D
Chemistry
. 2023 Sep;
29(67):e202302841.
PMID: 37665654
The Negishi cross-coupling reactions involves the application of organozinc reagents and is a highly versatile reaction in synthetic organic chemistry. The transmetallation step plays a pivotal role in the mechanism...
6.
Berthold D, van Otterlo W
Chemistry
. 2023 Jul;
29(61):e202302070.
PMID: 37515575
A general and concise synthetic pathway for the preparation of four different 5,8'-coupled naphthylisoquinoline alkaloids, employing a specially developed nickel/N,N-ligand-catalyzed atroposelective Negishi coupling is reported. In the first reported direct...
7.
Sabarwal A, van Rooyen J, Caburet J, Avgenikos M, Dheeraj A, Ali M, et al.
FASEB J
. 2022 Nov;
36(12):e22654.
PMID: 36421014
The therapeutic toxicity and resistance to currently available treatment options are major clinical challenges for the management of lung cancer. As a novel strategy, we synthesized analogues of a known...
8.
van der Westhuizen L, Weisner J, Taher A, Landel I, Quambusch L, Lindemann M, et al.
ChemMedChem
. 2022 Feb;
17(10):e202100776.
PMID: 35170857
Akt is a protein kinase that has been implicated in the progression of cancerous tumours. A number of covalent allosteric Akt inhibitors are known, and based on these scaffolds, a...
9.
Klintworth R, Morgans G, Scalzullo S, de Koning C, van Otterlo W, Michael J
Beilstein J Org Chem
. 2021 Nov;
17:2543-2552.
PMID: 34760023
A wide range of -(ethoxycarbonylmethyl)enaminones, prepared by the Eschenmoser sulfide contraction between -(ethoxycarbonylmethyl)pyrrolidine-2-thione and various bromomethyl aryl and heteroaryl ketones, underwent cyclization in the presence of silica gel to give...
10.
van der Westhuyzen A, Ingels A, Rosiere R, Amighi K, Oberer L, Gustafson K, et al.
Org Biomol Chem
. 2020 Oct;
18(40):8147-8160.
PMID: 33016969
The fungal metabolite sphaeropsidin A (SphA) has been recognised for its promising cytotoxicity, particularly towards apoptosis- and multidrug-resistant cancers. Owing to its intriguing activity, the development of SphA as a...