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Synthesis and Antiproliferative Activities of 1‐Hydroxyindole‐2‐Carboxylates
Author(s) -
Park Yeon Kyeong,
Ryu Yea Seong,
Cho Hyunsung,
Chung Ha Sook,
Lee Sang Hyup
Publication year - 2018
Publication title -
bulletin of the korean chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.237
H-Index - 59
ISSN - 1229-5949
DOI - 10.1002/bkcs.11418
Subject(s) - chemistry , oxalate , toluene , alcohol , chloride , thiol , cancer cell lines , combinatorial chemistry , cancer cell , organic chemistry , cancer , medicine
Synthesis and evaluation of antiproliferative activities of 1‐hydroxyindole‐2‐carboxylates 1 were described. The toluene compounds 3 were treated with dimethyl oxalate and then, dimethylmethyleneammonium chloride to give intermediates 2 . Compounds 2 were converted to desired compounds 1 by application of the reaction of 1‐hydroxyindole formation using SnCl 2 ·2H 2 O and thiol (or alcohol). The measurements of antiproliferative activities of compounds 1a , 1b , and 1c against several cell lines revealed that compounds 1a and 1c showed strong antiproliferative activities in HCT116 and A2058 cancer cells and could serve as promising lead compounds for further development of anticancer agents.