Niu, Haichan published the artcileStructure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization, Application In Synthesis of 86-51-1, the main research area is benzosuberene analog tubulin polymerization inhibitor vascular disrupting agent.
A promising design paradigm for small-mol. inhibitors of tubulin polymerization that bind to the colchicine site draws structural inspiration from the natural products colchicine and combretastatin A-4 (CA4). Our previous studies with benzocycloalkenyl and heteroaromatic ring systems yielded promising inhibitors with dihydronaphthalene and benzosuberene analogs featuring phenolic (KGP03 and KGP18; I and II, R = OH) and aniline (KGP05 and KGP156; I and II, R = NH2) congeners emerging as lead agents. These mols. demonstrated dual mechanism of action, functioning as both potent vascular disrupting agents (VDAs) and as highly cytotoxic anticancer agents. A further series of analogs was designed to extend functional group diversity and investigate regioisomeric tolerance. Ten new mols. were effective inhibitors of tubulin polymerization (IC50 < 5 μM) with seven of these exhibiting highly potent activity comparable to CA4, KGP18, and KGP03. For one of the most effective agents, dose-dependent vascular shutdown was demonstrated using dynamic bioluminescence imaging in a human prostate tumor xenograft growing in a rat. Journal of Medicinal Chemistry published new progress about 1,2-Addition reaction (1,2-addition/elimination reaction of benzosuberone derivative). 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Application In Synthesis of 86-51-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem