Combretastatin a-4 – Knowledge and References

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Molecular Photoswitches for Synthetic Optogenetics

Published in Francesco S. Pavone, Shy Shoham, Handbook of Neurophotonics, 2020

Other examples of interesting pharmacophores used in photoswitches include an anesthetic drug propofol (Stewart et al., 2011) in the design of AP2; a photoswitchable potentiator of GABAA-receptors (Stein et al., 2012). A clinically relevant drug combretastatin A-4 (Pettit et al., 1989) has been incorporated in a photoswitch designed to inhibit microtubule dynamics, denoted PST-1 (Figure 12.3f) (Borowiak et al., 2015) and a potassium-sparing diuretic drug, amiloride, was used in a photoamiloride switch called PA1 (Schonberger et al., 2014).

Binding affinity studies of 1,2,3-triazole copper(II) complexes to human serum albumin

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Journal Information

Published in Journal of Coordination Chemistry, 2018

Queite A. de Paula, Jean-Pierre Joly, Katalin Selmeczi, David E. P. Fonseca, Giovanni F. Caramori, Nicholas P. Farrell, Ana M. Da Costa Ferreira

Particularly, 1,2,3-triazole derivatives have been carefully investigated as powerful tools in studies related to angiogenesis inhibition and anticancer activities [16–18]. Also, a 4,5-disubstituted 2H-1,2,3-triazole analogue of natural combretastatin A-4 was evaluated against rat gliosarcoma cells, showing an LD50 value of 7.5 nM [19], and a few entered clinical trials, as a carboxyamido-triazole (CAI) [20], a nucleoside derivative (tert-butyldimethylsilylspiroaminooxathiole-dioxide (TSAO), a non-nucleoside inhibitor of reverse transcriptase activity) [21] and a β-lactamase inhibitor (Tazobactam®) [22].