Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 31181-89-2, is researched, Molecular C6H4ClNO, about Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells, the main research direction is carbamothioylamino pyridinylcarboxamide preparation diastereoselective antitumor activity docking SAR; Apoptosis; Cell cycle; Proliferation; Prostate cancer; Thiosemicarbazone.Reference of 5-Chloropicolinaldehyde.
To discover novel anticancer agents with potent and low toxicity, a range of new thiosemicarbazone-indole analogs I [R = H, Me, Cl, OMe; R1 = H, Me, R2 = H, Me, OH, etc.; R3 = H, Me; X = N, C] based on lead compound II were designed and synthesized previously. Most compounds displayed moderate to high anticancer activities against five tested tumor cells (PC3, EC109, DU-145, MGC803, MCF-7). Specifically, the represented compound I [R = H, R1 = Me; R2 = Me, R3 = H] (III) possessed strong antiproliferative potency and high selectivity toward PC3 cells with the IC50 value of 0.054μM, compared with normal WPMY-1 cells with the IC50 value of 19.470μM. Preliminary mechanism research indicated that compound (III) could significantly suppress prostate cancer cells (PC3, DU-145) growth and colony formation in a dose-dependent manner. Besides, derivative (III) induced G1/S cycle arrest and apoptosis, which may be related to ROS accumulation due to the activation of MAPK signaling pathway. Furthermore, mol. (III) could effectively inhibit tumor growth through a xenograft model bearing PC3 cells and had no evident toxicity in vivo. Overall, based on the biol. activity evaluation, analog (III) can be viewed as a potential lead compound for further development of novel anti-prostate cancer drug.
《Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(5-Chloropicolinaldehyde)Reference of 5-Chloropicolinaldehyde.
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Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate