Synthesis and biological evaluation of 3-amino-3-hydroxymethyloxindoles as potential anti-cancer agents

Kaili Jia; Xinxin Lv; Dong Xing; Jiuwei Che; Donglan Liu; Nilesh J. Thumar; Suzhen Dong; Wenhao Hu

doi:10.1039/c6ra27536b

Synthesis and biological evaluation of 3-amino-3-hydroxymethyloxindoles as potential anti-cancer agents

Kaili Jia
, Xinxin Lv
, Dong Xing
, Jiuwei Che
, Donglan Liu
, Nilesh J. Thumar
, Suzhen Dong^*
, Wenhao Hu

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

East China Normal University

Research output: Contribution to journal › Article › peer-review

15 Scopus citations

Abstract

A series of substituted 3-amino-3-hydroxymethyloxindoles (4a-4i) synthesized through a multi-component approach showed anticancer potency via in vitro cytotoxicity screening. Further, to develop the efficiency, derivatives (5a-5m) were synthesized and evaluated for their anti-proliferation activity. The most potent compound 5m showed cytotoxic effect toward SJSA-1 cells (IC₅₀ = 3.14 μM) as well as inhibiting the growth of other cancer cell lines (HCT-116, Jurkat, KB and Bel7402). Further investigation revealed that 5m induced a significant G2/M cell cycle arrest and time- and dose-dependent cellular apoptosis in SJSA-1 cells. These results suggested that new compound 5m has anti-proliferating and pro-apoptotic effects, which might be a candidate for cancer therapies.

Original language	English
Pages (from-to)	23265-23271
Number of pages	7
Journal	RSC Advances
Volume	7
Issue number	38
DOIs	https://doi.org/10.1039/c6ra27536b
State	Published - 2017

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title = "Synthesis and biological evaluation of 3-amino-3-hydroxymethyloxindoles as potential anti-cancer agents",

abstract = "A series of substituted 3-amino-3-hydroxymethyloxindoles (4a-4i) synthesized through a multi-component approach showed anticancer potency via in vitro cytotoxicity screening. Further, to develop the efficiency, derivatives (5a-5m) were synthesized and evaluated for their anti-proliferation activity. The most potent compound 5m showed cytotoxic effect toward SJSA-1 cells (IC50 = 3.14 μM) as well as inhibiting the growth of other cancer cell lines (HCT-116, Jurkat, KB and Bel7402). Further investigation revealed that 5m induced a significant G2/M cell cycle arrest and time- and dose-dependent cellular apoptosis in SJSA-1 cells. These results suggested that new compound 5m has anti-proliferating and pro-apoptotic effects, which might be a candidate for cancer therapies.",

author = "Kaili Jia and Xinxin Lv and Dong Xing and Jiuwei Che and Donglan Liu and Thumar, \{Nilesh J.\} and Suzhen Dong and Wenhao Hu",

note = "Publisher Copyright: {\textcopyright} 2017 The Royal Society of Chemistry.",

year = "2017",

doi = "10.1039/c6ra27536b",

language = "英语",

volume = "7",

pages = "23265--23271",

journal = "RSC Advances",

issn = "2046-2069",

publisher = "Royal Society of Chemistry",

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}

TY - JOUR

T1 - Synthesis and biological evaluation of 3-amino-3-hydroxymethyloxindoles as potential anti-cancer agents

AU - Jia, Kaili

AU - Lv, Xinxin

AU - Xing, Dong

AU - Che, Jiuwei

AU - Liu, Donglan

AU - Thumar, Nilesh J.

AU - Dong, Suzhen

AU - Hu, Wenhao

PY - 2017

Y1 - 2017

N2 - A series of substituted 3-amino-3-hydroxymethyloxindoles (4a-4i) synthesized through a multi-component approach showed anticancer potency via in vitro cytotoxicity screening. Further, to develop the efficiency, derivatives (5a-5m) were synthesized and evaluated for their anti-proliferation activity. The most potent compound 5m showed cytotoxic effect toward SJSA-1 cells (IC50 = 3.14 μM) as well as inhibiting the growth of other cancer cell lines (HCT-116, Jurkat, KB and Bel7402). Further investigation revealed that 5m induced a significant G2/M cell cycle arrest and time- and dose-dependent cellular apoptosis in SJSA-1 cells. These results suggested that new compound 5m has anti-proliferating and pro-apoptotic effects, which might be a candidate for cancer therapies.

AB - A series of substituted 3-amino-3-hydroxymethyloxindoles (4a-4i) synthesized through a multi-component approach showed anticancer potency via in vitro cytotoxicity screening. Further, to develop the efficiency, derivatives (5a-5m) were synthesized and evaluated for their anti-proliferation activity. The most potent compound 5m showed cytotoxic effect toward SJSA-1 cells (IC50 = 3.14 μM) as well as inhibiting the growth of other cancer cell lines (HCT-116, Jurkat, KB and Bel7402). Further investigation revealed that 5m induced a significant G2/M cell cycle arrest and time- and dose-dependent cellular apoptosis in SJSA-1 cells. These results suggested that new compound 5m has anti-proliferating and pro-apoptotic effects, which might be a candidate for cancer therapies.

UR - https://www.scopus.com/pages/publications/85021643953

U2 - 10.1039/c6ra27536b

DO - 10.1039/c6ra27536b

M3 - 文章

AN - SCOPUS:85021643953

SN - 2046-2069

VL - 7

SP - 23265

EP - 23271

JO - RSC Advances

JF - RSC Advances

IS - 38

ER -

Synthesis and biological evaluation of 3-amino-3-hydroxymethyloxindoles as potential anti-cancer agents

Abstract

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