Synthesis and bioevaluation of new vascular-targeting and anti-angiogenic thieno[2,3-d]pyrimidin-4(3H)-ones was written by Gold, Madeleine;Koehler, Leonhard;Lanzloth, Clarissa;Andronache, Ion;Anant, Shrikant;Dandawate, Prasad;Biersack, Bernhard;Schobert, Rainer. And the article was included in European Journal of Medicinal Chemistry in 2020.Formula: C8H6Br2O2 This article mentions the following:
A series of forty-six 5,6-annulated 2-arylthieno[2,3-d]pyrimidin-4(3H)-ones were prepared as potentially pleiotropic anticancer drugs with variance in the tubulin-binding trimethoxyphenyl motif at C-2 of a thieno[2,3-d]pyrimidine fragment, enlarged by addnl. rings of different size and substitution. By assessing their cytotoxicity against various cancer cells, their influence on the polymerization of neat tubulin and the dynamics of microtubule and F-actin cytoskeletons and their vascular-disrupting and anti-angiogenic activities in-vitro and in-vivo, structure-activity relations were identified which suggested the 3-iodo-4,5-dimethoxyphenyl substituted thienopyrimidine as a promising anticancer drug candidate for further research. In the experiment, the researchers used many compounds, for example, 3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1Formula: C8H6Br2O2).
3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Formula: C8H6Br2O2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary