An article Methylsulfanylpyridine based diheteroaryl isocombretastatin analogs as potent anti-proliferative agents WOS:000600418500067 published article about TUBULIN POLYMERIZATION INHIBITORS; COLCHICINE BINDING-SITE; PROTEIN-LIGAND DOCKING; COMBRETASTATIN A-4; STRUCTURAL BASIS; SOLID TUMORS; APOPTOSIS; DISCOVERY; GLUCURONIDATION; IDENTIFICATION in [Alvarez, Raquel; Aramburu, Laura; Vicente-Blazquez, Alba; Medarde, Manuel; Pelaez, Rafael] Univ Salamanca, Dept Ciencias Farmaceut, Lab Quim Organ & Farmaceut, Campus Miguel de Unamuno, E-37007 Salamanca, Spain; [Gajate, Consuelo; Vicente-Blazquez, Alba; Mollinedo, Faustino] CSIC, Dept Mol Biomed, Lab Cell Death & Canc Therapy, Ctr Invest Biol Margarita Salas, E-28040 Madrid, Spain; [Alvarez, Raquel; Aramburu, Laura; Vicente-Blazquez, Alba; Medarde, Manuel; Pelaez, Rafael] Univ Salamanca, Fac Farm, Inst Invest Biomed Salamanca IBSAL, Campus Miguel de Unamuno, E-37007 Salamanca, Spain; [Alvarez, Raquel; Aramburu, Laura; Vicente-Blazquez, Alba; Medarde, Manuel; Pelaez, Rafael] Univ Salamanca, Ctr Invest Enfermedades Trop Univ Salamanca CIETU, Campus Miguel de Unamuno, E-37007 Salamanca, Spain in 2021, Cited 65. HPLC of Formula: C8H8O2. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
Isocombretastatins are the not isomerizable 1,1- diarylethene isomers of combretastatins. Both families of antimitotics are poorly soluble and new analogs with improved water solubility are needed. The ubiquitous 3,4,5-trimethoxyphenyl ring and most of its replacements contribute to the solubility problem. 39 new compounds belonging to two series of isocombretastatin analogs with 2-chloro-6-methylsulfanyl-4-pyridinyl or 2,6-bis(methylsulfanyl)-4-pyridinyl moieties replacing the 3,4,5-trimethoxyphenyl have been synthesized and their antimitotic activity and aqueous solubility have been studied. We show here that 2-chloro-6-methylsulfanylpyridines are more successful replacements than 2,6-bis(methylsulfanyl) pyridines, giving highly potent tubulin inhibitors and cytotoxic compounds with improved water solubilities. The optimal combination is with indole rings carrying polar substitutions at the three position. The resulting diheteroaryl isocombretastatin analogs showed potent cytotoxic activity against human cancer cell lines caused by tubulin inhibition, as shown by in vitro tubulin polymerization inhibitory assays, cell cycle analysis, and confocal microscopy studies. Cell cycle analysis also showed apoptotic responses following G(2)/M arrest after treatment. Conformational analysis and docking studies were applied to propose binding modes of the compounds at the colchicine site of tubulin and were in good agreement with the observed SAR. 2-Chloro-6-methylsulfanylpyridines represent a new and successful trimethoxyphenyl ring substitution for the development of improved colchicine site ligands. (C) 2020 Elsevier Masson SAS. All rights reserved.
HPLC of Formula: C8H8O2. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Alvarez, R; Aramburu, L; Gajate, C; Vicente-Blazquez, A; Mollinedo, F; Medarde, M; Pelaez, R or concate me.
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles